Boronic acid and ester inhibitors of thrombin

ABSTRACT

Novel boronic acid and ester and carboxyl-modified amino acid compounds of the Formula I, which are inhibitors of trypsin-like enzymes, are disclosed: 
     
         R.sup.1 --Z--CHR.sup.2 --A, 
    
     where R 1 , Z, R 2  and A are defined within.

CROSS-REFERENCE TO EARLIER FILED APPLICATIONS

This application is a continuation-in-part of U.S. patent application Ser. No. 08/348/029, filed Dec. 1, 1994, still pending which is a continuation-in-part of U.S. patent application Ser. No. 08/318/029, filed Oct. 4, 1994, now abandoned which is a continuation-in-part of U.S. patent application Ser. No. 08/036/377, filed Mar. 24, 1993 now abandoned.

FIELD OF THE INVENTION

This invention relates to the discovery of new boronic acid derivatives which are inhibitors of thrombin and pharmaceutical compositions thereof.

BACKGROUND OF THE INVENTION

Hemostasis is the normal physiological process in which bleeding from an injured blood vessel is arrested. It is a dynamic and complex process in which proteolytic enzymes such as thrombin play a key role. Blood coagulation may occur through either of two cascades of zymogen activations, the extrinsic and intrinsic pathways of the coagulation cascade. Factor VIIa in the extrinsic pathway, and Factor IXa in the intrinsic pathway are important determinants of the activation of factor X to factor Xa, which itself catalyzes the activation of prothrombin to thrombin. The last protease in each pathway is thrombin, which acts to hydrolyze four small peptides (two FpA and two FpB) from each molecule of fibrinogen, thus deprotecting its polymerization sites. Once formed, the linear fibrin polymers may be cross-linked by factor XIIIa, which is itself activated by thrombin. In addition, thrombin is a potent activator of platelets, upon which it acts at specific receptors. Thrombin activation of platelets leads to aggregation of the cells and secretion of additional factors that further accelerate the creation of a hemostatic plug. Thrombin also potentiates its own production by the activation of factors V and VIII (see Hemker and Beguin in: Jolles, et. al., "Biology and Pathology of Platelet Vessel Wall Interactions," pp. 219-26 (1986), Crawford and Scrutton in: Bloom and Thomas, "Haemostasis and Thrombosis," pp. 47-77, (1987), Bevers, et. al., Eur. J. Biochem. 1982, 122, 429-36, Mann, Trends Biochem. Sci. 1987, 12, 229-33).

Thrombosis may be regarded as the pathological condition wherein improper activity of the hemostatic mechanism results in intravascular thrombus formation. Etiological factors such as the presence of atherosclerotic plaque, phlebitis and septicemia may cause thrombosis, leading to impaired blood flow to the effected tissues and possible serious pathological consequences. Thrombosis may be reduced by inhibition of the normal process of blood coagulation by anticoagulants. Anticoagulants act by reducing the amount of thrombin which is generated, or by inhibiting with the proteolytic actions of thrombin.

Currently, two of the most effective classes of drugs in clinical use as anticoagulants are the heparins and the vitamin K antagonists. The heparins are ill-defined mixtures of sulfated polysaccharides that bind to, and thus potentiate the action of antithrombin III. Antithrombin III is a naturally occurring inhibitor of the activated clotting factors Ixa, Xa, XIa, thrombin and probably XIIa (see Jaques, Pharmacol. Rev. 1980, 31, pp. 99-166). The vitamin K antagonists, of which warfarin is the most well-known example, act indirectly by inhibiting the post-ribosomal carboxylations of the vitamin K dependent coagulation factors II, VII, IX and X (see Hirsch, Semin. Thromb. Hemostasis 1986, 12, 1-11). While effective therapies for the treatment of thrombosis, heparins and vitamin K antagonists have the unfortunate side effects of bleeding and marked interpatient variability, resulting in a small and unpredictable therapeutic safety margin. The use of direct acting thrombin inhibitors is expected to alleviate these problems.

Anticoagulants are also necessary in the processing of blood for therapeutic or diagnostic purposes or for the production of blood products or fragments, since contact of blood with the surfaces commonly used for blood collection and storage causes activation of coagulation leading to thrombin formation and clot formation.

The coagulation proteases thrombin, factor Xa, factor VIIa, and factor IXa are serine proteases having trypsin-like specificity for the cleavage of sequence-specific Arg-Xxx peptide bonds. As with other serine proteases, the cleavage event begins with an attack of the active site serine on the scissile bond of the substrate, resulting in the formation of a tetrahedral intermediate. This is followed by collapse of the tetrahedral intermediate to form an acyl enzyme and release of the amino terminus of the cleaved sequence. Hydrolysis of the acyl enzyme then releases the carboxy terminus.

A number of naturally occurring thrombin inhibitors have been reported. These include nazumamide A from Theonella sp. (see Fusetani, et. al., Tetrahedron Lett. 1991, 32, 7073-4), cyclotheonamide A from Theonella sp. (see Fusetani, et. al., J. Am. Chem. Soc. 1990, 112, 7053-4), amblyommin from Amblyomma hebraeum (see Bonin, et. al., EP 345614), hirudin from Hirudo medicinalis, recombinant versions of hirudin and hirudin fragments (see Rigbl and Jackson, EP 352903, Koerwer, WO 9109946, Meyer, et. al., WO 9108233, Dawson, et. al., WO 9109125, Maraganore, et. al., WO 9102750 and Maraganore, EP 33356).

Synthetic thrombin inhibitors have also been disclosed. Arylsulfonylarginine amides such as (2R,4R)-4-methyl-1-[N² -{(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl) sulfonyl}-L-arginyl]-2-piperidinecarboxylate have been shown to be effective inhibitors of thrombin (see Okamoto, et. al. Thromb Res. 1976, 8, 77-82, Ohshiro, et. al., Blood Vessel 1983, 14, 216-8), as have compounds containing constrained arginine mimics such as (2-naphthylsulfonylglycyl)-4-amidino-phenylalanyl piperidide (see Stuerzebecher, et. al., Thromb. Res. 1983, 29, 635-42), 1-[2-[5-(dimethylamino)naphth-1-ylsulfonamido]-3-(2-iminohexahydropyrimidin-5-yl)propanoyl]-4-methylpiperidine dihydrochloride (see Ishikawa, JP 88227572 and Ishikawa and Inamura, JP 88227573), N-(trans-4-amino-methylcyclohexylcarbonyl)-4-O-(2-picolyl)-L-tyrosine 4-acetanilide dihydrochloride (see Okamoto, et. al., EP 217286) and 4-[(aminoiminomethyl)amino]benzoic acid esters (see Fuji, et. al., DE 3005580, Matsuoka, et. al., Jpn. J. Pharmacol. 1989, 51, 455-63, and Takeshita, et. al., EP 435235).

Inhibitor design has benefitted from the knowledge of the mechanism of action and of the peptide sequences which are thought to bind in the catalytic site of thrombin, e.g., -Gly-Val-Arg-Gly- of fibrinogen (see Blomb ack, et. al., J. Biol. Chem., 1972, 247, 1496-512), Ile-Pro-Arg-Ser- of prothrombin (see Magnussen, et. al., in: Reich, et. al., "Proteases and Biological Control," pp. 123-149 (1975)) and -Val-Pro-Arg-Gly- of factor XIII (see Takagi and Doolittle, Biochemistry 1974, 13, 750-6 and Nakamura, et. al., Biochem. Biophys. Res. Commun. 1974, 58, 250-256). This class of mechanism-based inhibitors are exemplified by the tripeptide aldehyde D-Phe-Pro-N-Me-Arg-H (see Bajusz, et. al., J. Med. Chem. 1990, 33, 1729-35), the chloromethyl ketone Ac-D-Phe-Pro-ArgCH₂ Cl (see Kettner and Shaw, Thromb. Res. 1979, 14, 969-73) and the trifluoromethyl ketone D-Phe-Pro-ArgCF₃ (see Kolb, et. al., US 697987).

Kettner and Shenvi (EP 293881, published Jun. 12, 1988), disclose peptide boronic acid inhibitors of trypsin-like proteases of formula (1)

    R.sup.1 -[(A.sup.3).sub.q (A.sup.2).sub.p (A.sup.1).sub.o ].sub.n --NH--CHR.sup.2 --BY.sup.1 Y.sup.2                        ( 1)

wherein Y¹ and Y², independently, are hydroxyl or fluoro or, taken together, form a moiety derived from a dihydroxy compound having at least two hydroxy groups separated by at least two connecting atoms in a chain or ring, said chain or ring comprising 1 to about 20 carbon atoms and, optionally, a heteroatom which can be N, S, or O; R² is a substituted alkyl selected from the group consisting of --(CH₂)_(z) --X, --(CH(CH₃)--(CH₂)₂ --X, --CH₂ --CH--(CH₃)--CH₂ --X, --(CH₂)₂ --CH(CH₃)--X and --(CH₂)₂ --CH(CH₃)₂ --X, where X is --NH₂, --NH--C(NH)--NH₂ or --S--C(NH)--NH₂, and z is 3 to 5; n, o, p and q are, independently, either 0 or 1; A¹, A² and A³ are, independently, amino acids of L- or D-configuration selected from the group consisting of Ala, Arg, Ash, Asp, Cys, Gln, Glu, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr and Val; and R¹ is a peptide comprised of 1 to about 20 amino acids, an acyl or a sulfonyl group comprised of 1 to about 20 carbon atoms, H, or an N-terminal protecting group. In this disclosure, Kettner and Shenvi demonstrated that the pinanediol esters of boropeptides are pharmacogolically equivalent to the corresponding boronic acids.

Metternich (EP 0471651 A2) discloses borolysine thrombin inhibitors of formula (2)

    W--Y--NR.sup.4 --CHR.sup.5 --BQ.sup.1 Q.sup.2              ( 2)

wherein W is an N-protecting group; Y is a sequence of n amino acids such that the n+1 amino acid peptide Y-Lys or Y-Arg has an affinity for the active site of a trypsin-like protease; where n is an integer of from 1 to 10 and in which at least one amino acid is an unnatural amino acid having a hydrophobic side chain; Q¹ and Q² are the same or different and are selected from --OH, --COR₁, --CONR₁ R₂, --NR₁ R₂ or --OR₃ of Q¹ and Q² taken together form a diol residue; R₁, R₂ and R₃ which may be the same or different, are C₁₋₁₀ alkyl, C₆₋₁₀ aryl, C₆₋₁₀ aralkyl, or phenyl substituted by up to three groups selected from C₁₋₄ alkyl, halogen and C₁₋₄ alkoxy; R₄ is hydrogen or C₁₋₁₀ alkyl; R₅ is a group --A--X; wherein A is --(CH₂)_(z) -- in which z is 2, 3, 4 or 5; --CH(CH₃)--(CH₂)₂ --; --CH₂ --CH(CH₃)--CH₂ --; --(CH₂)₂ --CH(CH₃)--; --(CH₂)₂ --C(CH₃) ₂ --; CH(CH₃)--(CH₂)₃ --; --CH₂ --CH(CH₃)--(CH₂)₂ --; --CH₂ --CH₂ --CH (CH₃)--CH₂ --; --(CH₂)₃ --CH(CH₃)--; --(CH₂)₃ --C(CH₃)₂ : C₆₋₁₀ aryl C₆₋₁₀ aralkyl and X is --NH₂, --NH--C(NH)--NH₂, --S--C(NH)--NH₂, N₃, --C₁₋₄ alkoxy, C₁₋₄ alkylthio or Si(CH₃)₃ or R₄ and R₅ taken together form a trimethylene group and the asymmetric carbon atom may have the D- or L-configuration or represent any mixture of these.

Surprising for their lack of a basic residue at P₁ are tripeptide thrombin inhibitors comprised of 1-aminoboronic and 1-aminophosphonic acid analogs of 3-methoxy-propylglycine (see Claeson, et. al., U.S. Pat. No. 07-245428) and pentylglycine (see Cheng, et. al., "Symposium on Thrombosis and Hemostasis," 1991, Amsterdam, Abstract 2150).

In addition to thrombin inhibition, boropeptides have been disclosed with utility as a treatment for tumors, viral infections and arthritis (U.S. Pat. No. 4963655A and EP 354522A), emphysema (U.S. Pat. No. 4499082A), hypertension (EP 315574A) and as factor VII/VIIa inhibitors (WO 8909612A). Kleemann, et. al. (AU A-24693/88) disclose renin-inhibiting 1-amino boronic acid derivatives of formula (3)

    A.sup.1 --A.sup.2 --HN--CHR.sup.2 --BXR.sup.3 (YR.sup.4)   (3)

in which A¹ denotes a radical of formulae (4-8).

    R.sup.1 NR.sup.6 --CHR.sup.5 --C═O--                   (4)

    R.sup.1 CHR.sup.12 --CHR.sup.5 --C═O--                 (5)

    R.sup.1 NR.sup.6 --CHR.sup.5 --CHR.sup.7 --CHR.sup.8 --CHR.sup.9 --C═O--(6)

    R.sup.1 CHR.sup.12 --CHR.sup.5 --CHR.sup.7 --CHR.sup.8 --CHR.sup.9 --C═O--                                               (7)

    R.sup.10 --(CH.sub.2).sub.n --CH(CH.sub.2).sub.m R.sup.11 --C═O--(8)

Despite the foregoing, more efficacious and specific inhibitors of coagulation proteases are needed as potentially valuable therapeutic agents for the treatment of thrombosis. None of the cited references describe or suggest the new thrombin-inhibiting boronic acid derivatives of the present invention.

SUMMARY OF INVENTION

This invention pertains to novel compounds of formula (I):

    R.sup.1 --Z--CHR.sup.2 --A                                 (I)

wherein

A is

a) --BY¹ Y²,

b) --C(═O)CF₃,

c) --C(═O)CHF₂,

d) --C(═O)CH₂ F,

e) --C(═O)CH₂ Cl,

f) --C(═O)OR³,

g) --C(═O)NR¹⁵ R¹⁶,

h) --C(═O)R³,

i) --C(═O)COOR³,

j) --C(═O)C(═O)NR¹⁵ R¹⁶,

k) --C(═O)C(═O)R³,

l) --C(═O)CY³ Y⁴ COOR³,

m) --C(═O)CY³ Y⁴ C(═O)NR¹⁵ R¹⁶,

n) --C (═O)CY³ Y⁴ C(═O)R³,

o) --PO₃ H₂, or

p) --CHO;

Y¹ and Y² are independently

a) --OH,

b) --F,

c) --NR³ R⁴, or

d) C₁ -C₈ alkoxy;

Y¹ and Y² can be taken together to form:

e) a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O,

f) a cyclic boron amide where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O,

g) a cyclic boron amide-ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O;

Y³ and Y⁴ are independently

a) --OH or

b) --F;

Z is

a) --(CH₂)_(m) CONR⁸ --,

b) --(CH₂)_(m) CSNR⁸ --,

c) --(CH₂)_(m) SO₂ NR⁸ --,

d) --(CH₂)_(m) CO₂ --,

e) --(CH₂)_(m) C(S)O--, or

f) --(CH₂)_(m) SO₂ O--;

R¹ is

a) --(CH₂)_(p) -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents selected from the group consisting of:

halo(F, Cl, Br, I), methylenedioxy, --R⁸, --NR⁸ COR⁹, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, --(CH₂)_(w) --OR⁸, --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CHO; --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹. --(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ --perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO-(phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO₂ -(phenyl), --O(C═O)--(C₁ -C₅ -alkyl), ##STR1## b) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted:

i) quinolinyl,

ii) isoquinolinyl,

iii) benzopyranyl,

iv) benzothiophenyl,

v) benzofuranyl,

vi) 5,6,7,8-tetrahydroquinolinyl,

vii) 5,6,7,8-tetrahydroisoquinolinyl,

and wherein the substituents are selected from the group consisting of halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, R⁸, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --C0NHR⁸, NR⁸ COR⁹, NR⁸ CO₂ R⁹, ##STR2## wherein J is N or C and K, L, M and Q are independently selected at each occurrence from the group consisting of N, CR¹³, S or O, provided that:

i) there may be only one S or O present in the ring at a time;

ii) there may only be 1-2N present when there is an O or S present;

iii) there may be only 1-4N present; g) ##STR3## wherein W, R, T, U and V are selected from the group consisting of: CR¹³ or N, provided that there be no less than 1 and no more than 3N present; ##STR4## is as defined above; ##STR5## is as defined above; ##STR6## wherein G is O, S, or NP, where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³); ##STR7## wherein G is O, S, or NP, where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³);

R² is

a) --(C₁ -C₁₂ alkyl)--X,

b) --(C₂ -C₁₂ alkenyl)--X, or ##STR8## X is a) halogen (F, Cl, Br, I),

b) --CN,

c) --NO₂,

d) --CF₃,

e) --S(O)_(r) R¹⁴,

f) --NHR¹⁴

g) --NHS(O)_(r) R¹⁴,

h) --NHC(NH)H,

i) --NHC(NH)NHOH,

j) --NHC(NH)NHCN,

k) --NHC(NH)NHR¹⁴,

l) --NHC(NH)NHCOR¹⁴,

m) --C(NH)NHR¹⁴,

n) --C(NH)NHCOR¹⁴,

o) --C(O)NHR¹⁴,

p) --C(O)NHC(O)R¹⁴,

q) --C(O)OR¹⁴,

r) --OR¹⁴,

s) --OC(O)R¹⁴,

t) --OC(O)OR¹⁴,

u) --OC(O)NHR¹⁴,

v) --OC(O)NHC(O)R¹⁴,

w) --SC(═NH)NHR¹⁴, or

x) --SC(═NH)NHC(═O)R¹⁴ ;

R³ is

a) hydrogen,

b) C₁ -C₈ alkyl,

c) --(C₁ -C₄ alkyl )-aryl,

d) C₅ -C₇ cycloalkyl, or

e) phenyl;

R⁴ is

a) hydrogen,

b) C₁ -C₈ alkyl,

c) --(C₁ -C₄ alkyl)-aryl,

d) C₅ -C₇ cycloalkyl,

e) phenyl, or

f) phenylsulfonyl;

R⁵ and R⁶ are hydrogen or when taken together form a six membered aromatic ring optionally substituted with one, two or three substituents selected from the group consisting of halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONR⁸ R⁹, phenyl, benzyl, phenylethyl;

R⁷ is

a) phenyl,

b) C₁ -C₈ -alkyl,

c) C₁ -C₄ -alkoxy,

d) --CF₃, or

e) benzyl;

R⁸ and R⁹ are independently

a) H, ##STR9## c) C₃ -C₇ cycloalkyl, or d) C₁ -C₈ -alkyl;

R¹¹ is

a) halo (F, Cl, Br, I),

b) --CN,

c) C₁ -C₁₀ -alkyl,

d) C₃ -C₈ -cycloalkyl,

e) C₂ -C₁₀ -alkenyl,

f) C₂ -C₁₀ -alkynyl,

g) --OR⁸,

h) --NO₂,

i) --CF₃,

j) --S(O)_(r) R⁷,

k) --NR⁸ R⁹,

l) --COR⁹,

m) --CO₂ R⁸,

n) --CONR⁸ R⁹, or

o) H

R¹² is

H, C₁ -C₄ alkyl, phenyl, benzyl, --COR⁷, or --S(O)_(r) R⁷ ;

R¹³ is

H, halogen (F, Cl, Br, I), (C₁ -C₈)alkyl, (C₁ -C₆)-perfluoroalkyl, --(CH₂)_(r) --D, C₃ -C₈ cycloalkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, methylenedioxy, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) NC, --(CH₂)_(w) CN, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ -(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ -(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO₂ -(phenyl), --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, --S--(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, or --O--(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸ ;

R¹⁴ is

a) --H,

b) --CF₃

c) --C₁ -C₄ alkyl,

d) --(CH₂)_(q) -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl unsubstituted or substituted with one to three substituents selected from the group consisting of:

halogen (F, Cl, Br, I),

--CF₃,

--(C₁ -C₄ alkyl),

--(CH₂)_(x) R¹⁵,

--(CH₂)_(x) CO(CH₂)_(y) R¹⁵,

--(CH₂)_(x) C(O)O(CH₂)_(y) R¹⁵,

--(CH₂)_(x) C(O)N[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ],

--methylenedioxy,

--(C1-C4 alkoxy),

--(CH₂)_(x) O(CH₂)_(y) R¹⁵,

--(CH₂)_(x) OCO(CH₂)_(y) R¹⁵,

--(CH₂)_(x) OC(O)O(CH₂)_(y) R¹⁵,

--(CH₂)_(x) OC(O)N[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ],

--(CH₂)_(x) OC(O)N[(CH₂)_(y) R¹⁵ ] [CO (CH₂)_(y) R¹⁶ ],

--(CH₂)_(x) S(O)_(r) (CH₂)_(y) R¹⁵,

--(CH₂)_(x) S(O)_(r) (CH₂)_(y) COR¹⁵,

--(CH₂)_(x) S(O)_(r) (CH₂)_(y) C(O)OR¹⁵,

--(CH₂)_(x) S(O)_(r) N[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ]

--(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ],

--(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ] [CO(CH₂)_(y) R¹⁶ ],

--(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ] [C(O)O(CH₂)_(y) R¹⁶ ],

--(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ]CON[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ],

--(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ]CON[(CH₂)_(y) R¹⁵ ] [CO(CH₂)_(y) R¹⁶ ],

--(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ] [S(O)_(r) (CH₂)_(y) R¹⁶ ];

R¹⁵ and R¹⁶ are independently

a) hydrogen,

b) C₁ -C₈ alkyl,

c) --(C₁ -C₄ alkyl)-aryl, where aryl is defined above,

d) C₅ -C₇ cycloalkyl,

e) phenyl, substituted by 0-3 R¹⁸,

f) benzyl, substituted by 0-3 R¹⁸, or

g) --(C₁ -C₄ alkoxy);

R¹⁵ and R¹⁶ can be taken together to form a ring: ##STR10## R¹⁸ and R¹⁹ are independently H, halo (F, Cl, Br, I), C₁ -C₈ -alkyl, C₃ -C₈ cycloalkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ -(C₁ -C₆)--perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(C═O )--(C₁ -C₅ -alkyl), --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -phenyl), or --O(C═O)phenyl;

R18 and R19 can be taken together to form a methylenedioxy group;

R²⁰ and R^(20a) are independently

(C₁ -C₈)alkyl, --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, (C₁ -C₆)-perfluoroalkyl, or --(CH₂)_(r) --D;

m is 0 to 6;

n is 1 to 2;

p is 0 to 2;

q is 0 to 4.

r is 0 to 2;

s is 0 to 3;

t is 1 to 5;

u is 0 to 5;

v is 0 to 5;

w is 0 to 5;

x is 0 to 6;

y is 0 to 6;

D is fur-2-yl, fur-3-yl, thiophen-2-yl, thiophen-3-yl, oxazol-2-yl, oxazol-4-yl, thiazol-2-yl, thiazol-4yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, pyrid-2-yl, pyrid-4-yl, pyridazin-3-yl, pyridazin-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrazin-2-yl, or tetrazolyl;

E is --CO--, --SO₂ --, --CH₂ -- or a single bond;

F is --CO--;

W is

a) --O--,

b) --S(O)_(r) --,

c) --NR⁴ --,

d) --NC(═O)R³ --,

e) a bond, or

f) --(CH₂)_(n) --;

or prodrugs or pharmaceutically acceptable salts thereof.

Preferred compounds of formula (I) are those compounds wherein:

Z is

a) --(CH₂)_(m) CONR⁸ --,

b) --(CH₂)_(m) CSNR⁸ --,

c) --(CH₂)_(m) SO₂ NR⁸ --,

R¹ is

a) --(CH₂)_(p) -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents selected from the group consisting of:

halo (F, Cl, Br, I), methylenedioxy, --R⁸, --NR⁸ COR⁹, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, --(CH₂)_(w) --OR⁸, --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹. --(CH₂)_(w) SO₂ NH--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO-(phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -perfluoroalkyl), or --(CH₂)_(w) NH--CO₂ -(phenyl),--O(C═O--(C₁ -C₅ alkyl);

b) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted:

i) quinolinyl,

ii) isoquinolinyl,

iii) benzopyranyl,

iv) benzothiophenyl,

v) benzofuranyl,

vi) 5,6,7,8-tetrahydroquinolinyl,

vii) 5,6,7,8-tetrahydroisoquinolinyl,

and wherein the substituents are selected from the group consisting of halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, R⁸, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONR⁸ H, NR⁸ COR⁹, NR⁸ CO₂ R⁹ ; ##STR11## f) wherein the ring ##STR12## represented by --J--K--L--M--Q-- is a group selected from: 1) --N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,

2) --N--C(R¹³)═C(R¹³)--C(R¹³)═N--,

3) --N--C(R¹³)═C(R¹³)--N═C(R¹³)--,

4) --N--C(R¹³)═N--C(R¹³)═N--,

5) --N--C(R¹³)═C(R¹³)--N═N--

6) --N--C(R¹³)═N--N═N--,

7) --N--N═C(R¹³)--N═N--,

8) ═C--O--C(R¹³)═N--C(R¹³)═,

9) --C═C(R¹³)--O--C(R¹³)═N--,

10) ═C--O--C(R¹³)═C(R¹³)--N═,

11) --C═C(R¹³)--C(R¹³)═N--O--,

12) ═C--C(R¹³)═C(R¹³)--O--N═,

13) --C═C(R¹³)--O--N═C(R¹³)--,

14) ═C--S--C(R¹³)═N--C(R¹³)═,

15) --C═C(R¹³)--S--C(R¹³)═N--,

16) ═C--S--C(R¹³)═C(R¹³)--N═,

17) --C═N--S--N═C(R¹³)--,

18) --C═N--S--C(R¹³)═N--,

19) ═C--S--N═C(R¹³)--N═,

20) ═C--S--C(R¹³)═C(R¹³)--C(R¹³)═,

21) --C═C(R¹³)--S--C(R¹³)═C(R¹³)--,

22) ═C--O--C(R¹³)═C(R¹³)--C(R¹³)═, or

23) --C═C(R¹³)--O--C(R¹³)═C(R¹³)--;

g) wherein the ring ##STR13## represented by --C--W--R--T--U--V-- is a group selected from: 1) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,

2) --C═C(R¹³)--N═C(R¹³)--C(R¹³)═C(R¹³)--,

3) --C═C(R¹³)--C(R¹³)═N--C(R¹³)═C(R¹³)--,

4) --C═N--N═C(R¹³)--C(R¹³)═C(R¹³)--,

5) --C═C(R¹³)--N═N--C(R¹³)═C(R¹³)--,

6) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═N--,

7) --C═N--C(R¹³)═C(R¹³)--N═C(R¹³)--,

8) --C═N--C(R¹³)═N--C(R¹³)═C(R¹³)--,

9) --C═C(R¹³)--N═C(R¹³)--N═C(R¹³)--,

10) --C═N--C(R¹³)═N--N═C(R¹³)--,

11) --C═N--C(R¹³)═C(R¹³)--N═N--, or

12) --C═C(R¹³)--N═C(R¹³)--N═N--; ##STR14## is as defined above; ##STR15## is as defined above; ##STR16## wherein G is O, S; or NP (where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³ ; ##STR17## wherein G is O, S, or NP (where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³ ;

R¹⁴ is

a) --H,

b) --CF₃

c) --C₁ -C₄ alkyl,

d) --(CH₂)_(q) -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl unsubstituted substituted with one to three substituents selected from the group consisting of:

halogen (F, Cl, Br, I),

--CF₃,

--(C₁ -C₄ alkyl),

--methylenedioxy,

--(C₁ -C₄ alkoxy),

--(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ];

and all other required substituents of formula (I) are as defined in claim 1.

More preferred compounds of the formula (I) are those compounds wherein:

A is

a) --BY¹ Y²,

b) --C(═O)CF₃,

c) --C(═O)CHF₂,

d) --C(═O)CH₂ F,

e) --C(═O)CH₂ Cl,

f) --C(═O)OR³,

g) --C(═O)NR¹⁵ R¹⁶,

h) --C(═O)R³,

i) --C(═O)COOR³,

j) --C(═O)C(═O)NR¹⁵ R¹⁶,

k) --C(═O)C(═O)R³,

l) --CHO;

Y¹ and Y² are independently

a) --OH, or

b) C₁ -C₈ alkoxy;

Y¹ and Y² can be taken together to form a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O,

Z is

a) --(CH₂)_(m) CONR⁸ --,

b) --(CH₂)_(m) CSNR⁸ --, or

c) --(CH₂)_(m) SO₂ NR⁸ --;

R¹ is

a) --(CH₂)_(p) -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents independently selected at each occurrence from the group consisting of:

halo (F, Cl, Br, I), methylenedioxy, --R⁸, --NR⁸ COR⁹, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, --(CH₂)_(w) --OR⁸, --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹. --(CH₂)_(w) SO₂ NH--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -perfluoroalkyl), or --(CH₂)_(w) NH--CO₂ -(phenyl), --O(C═O)--C₁ -C₅ -alkyl);

b) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted:

i) quinolinyl,

ii) isoquinolinyl,

iii) benzopyranyl,

iv) benzothiophenyl,

v) benzofuranyl,

vi) 5,6,7,8-tetrahydroquinolinyl,

vii) 5,6,7,8-tetrahydroisoquinolinyl,

wherein the substituents are members selected from the group consisting of: halo (F, Cl, Br, I), --CN, C₁ 14 C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, R⁸, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONR⁸ H, NR⁸ COR⁹, NR⁸ CO₂ R⁹ ; ##STR18## wherein the ring represented by --J--K--L--M--Q-- is a group selected from:

1) --N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,

2) --N--C(R¹³)═C(R¹³)--C(R¹³)═N--,

3) --N--C(R¹³)═C(R¹³)--N═C(R¹³)--,

4) --N--C(R¹³)═N--C(R¹³)═N--,

5) --N--C(R¹³)═C(R¹³)--N═N--

6) --N--C(R¹³)═N--N═N--,

7) --N--N═C(R¹³)--N═N--,

8) ═C--O--C(R¹³)═N--C(R¹³)═,

9) --C═C(R¹³)--O--C(R¹³)═N--,

10) ═C--O--C(R¹³)═C(R¹³)--N═,

11) --C═C(R¹³)--C(R¹³)═N--O--,

12) ═C--C(R¹³)═C(R¹³)--O--N═,

13) --C═C(R¹³)--O--N═C(R¹³)--,

14) ═C--S--C(R¹³)═N--C(R¹³)═,

15) --C═C(R¹³)--S--C(R¹³)═N--,

16) ═C--S--C(R¹³)═C(R¹³)--N═,

17) ═C--S--C(R¹³)═C(R¹³)--C(R¹³)═,

18) --C═C(R¹³)--S--C(R¹³)═C(R¹³)--,

19) ═C--O--C(R¹³)═C(R¹³)--C(R¹³)═, or

20) --C═C(R¹³)--O--C(R¹³)═C(R¹³)--; ##STR19## wherein the ring represented by --C--W--R--T--U--V-- is a group selected from:

1) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,

2) --C═C(R¹³)--N═C(R¹³)--C(R¹³)═C(R¹³)--,

3) --C═C(R¹³)--C(R¹³)═N--C(R¹³)═C(R¹³)--,

4) --C═N--N═C(R¹³)--C(R¹³)═C(R¹³)--,

5) --C═C(R¹³)--N═N--C(R¹³)═C(R¹³)--,

6) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═N--,

7) --C═N--C(R¹³)═C(R¹³)--N═C(R¹³)--,

8) --C═N--C(R¹³)═N--C(R¹³)═C(R¹³)--,

9) --C═C(R¹³)--N═C(R¹³)--N═C(R¹³)--,

10) --C═N--C(R¹³)═N--N═C(R¹³)--,

11) --C═N--C(R¹³)═C(R¹³)--N═N--, or

12) --C═C(R¹³)--N═C(R¹³)--N═N--; ##STR20## is as defined above; ##STR21## is as defined above; or ##STR22## wherein G is O, S, or NP (where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³);

R² is

a) --(C₁ -C₁₂ alkyl)--X,

b) --(C₂ -C₁₂ alkenyl )--X, or ##STR23## X is a) halogen (F, Cl, Br, I),

b) --CN,

c) --NO₂,

d) --CF₃,

e) 13 NHR¹⁴

f) --NHS(O)_(r) R¹⁴,

g) --NHC(NH)H,

h) --NHC(NH)NHOH,

i) --NHC(NH)NHCN,

j) --NHC(NH)NHR¹⁴,

k) --NHC(NH)NHCOR¹⁴,

l) --C(NH)NHR¹⁴,

m) --C(NH)NHCOR¹⁴,

n) --C(O)NHR¹⁴,

o) --C(O)NHC(O)R¹⁴,

p) --C(O)OR¹⁴,

q) --OR¹⁴,

r) --OC(O)R¹⁴,

s) --OC(O)OR¹⁴,

t) --OC(O)NHR¹⁴,

u) --OC(O)NHC(O)R¹⁴,

v) --SC(═NH)NHR¹⁴, or

w) --SC(═NH)NHC(═O)R¹⁴ ;

R¹³ is

H, halogen (F, Cl, Br, I), (C₁ -C₆)alkyl, --(CH₂)_(r) --D, methylenedioxy, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) NC, --(CH₂)_(w) CN, --(CH₂)_(w) NO₂, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -phenyl), --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, or --O(C═O)phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸ ;

R¹⁴ is

a) --H,

b) --CF₃

c) --C1-C4 alkyl,

d) --(CH₂)_(q) -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl are optionally substituted with one to three substituents selected from the group consisting of:

halogen (F, Cl, Br, I),

--CF₃,

--(C1-C4 alkyl),

--methylenedioxy,

--(C1-C4 alkoxy), or

--(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ];

R¹⁸ and R¹⁹ are independently

H, halo (F, Cl, Br, I), C₁ -C₆ -alkyl, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -phenyl), or --O(C═O)phenyl;

R18 and R19 can be taken together to form a methylenedioxy group;

R²⁰ and R^(20a) are independently (C₁ -C₈)alkyl, --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, (C₁ -C₆)-perfluoroalkyl, or --(CH₂)_(r) --D;

D is fur-2-yl, fur-3-yl, thiophen-2-yl, thiophen-3-yl, oxazol-2-yl, oxazol-4-yl, thiazol-2-yl, thiazol-4-yl, pyrid-2-yl, pyrid-4-yl, pyrimidin-2-yl, or pyrimidin-4-yl;

W is

a) --O--,

b) --NR⁴ --,

c) a bond, or

d) --(CH₂)_(n) --;

and all other required substituents of formula (I) are as defined in claim 2.

Most preferred compounds of the formula (I) are those compounds wherein:

A is --BY¹ Y² ;

Y¹ and Y² are --OH;

Y¹ and Y² can be taken together to form a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O,

Z is --(CH₂)_(m) CONR⁸ --;

R¹ is

a) --(CH₂)_(p) -aryl, wherein aryl is phenyl, naphthyl or biphenyl substituted with one, two or three substituents selected from the group consisting of:

halo (F, Cl, Br, I), methylenedioxy, --R⁸, --NR⁸ COR⁹, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, --(CH₂)_(w) --OR⁸, --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹. --(CH₂)_(w) SO₂ NH--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -perfluoroalkyl), or --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -phenyl);

b) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted isoquinolinyl wherein the substituents are members selected from the group consisting of:

halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ ∝C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, R⁸, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONR⁸ R⁹, NR⁸ COR⁹, NR⁸ CO₂ R⁹, ##STR24## wherein the ring represented by --J--K--L--M--Q-- is a group selected from:

1) --N--C(R¹³)═N--C(R¹³)═N--,

2) --N--C(R¹³)═C(R¹³)--N═N--,

3) --N--N═C(R¹³)--N═N--,

5) --N--C(R¹³)═N--N═N--,

6) ═C--S--C(R¹³)═C(R¹³)--C(R¹³)═, or

7) ═C--O--C(R¹³)═C(R¹³)--C(R¹³)═; ##STR25## wherein the ring represented by --C--W--R--T--U--V-- is a group s elected from:

1) --C═N--C(R¹³)═C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--

1) --C═C(R¹³)--N═C(R¹³)--C(R¹³)═C(R¹³)--,

2) --C═C(R¹³)--C(R¹³)═N--C(R¹³)═C(R¹³)--,

3) --C═C(R¹³)--N═C(R¹³)--N═C(R¹³)--,

4) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═N--, or

5) --C═N--C(R¹³)═N--C(R¹³)═C(R¹³)--; ##STR26## is as defined above; ##STR27## is as defined above; or ##STR28## wherein G is S; R² is

a) --(C1-C12 alkyl)--X, or ##STR29## X is a) halogen (F, Cl, Br, I),

b) --CN,

c) --NHR¹⁴

d) --NHC(NH)H,

e) --NHC(NH)NHR¹⁴,

f) --C(NH)NHR¹⁴,

g) --OR¹⁴, or

h) --SC(═NH)NHR¹⁴ ;

R¹¹ is H;

R¹³ is

H, halogen (F, Cl, Br, I), --(CH₂)_(w) NO₂, (C₁ -C₆)alkyl, --(CH₂)_(r) --D, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CO₂ R³, --(CH₂)_(w) NR⁸ R³, --(CH₂)_(w) S(O)₂ R⁷, --(CH2wSO2NHCO--(C1-C6)-alkyl, --(CH2)wNHSO2-phenyl --(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂ )_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) CN₄ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(t) CN, --NH(CH₂)_(t) CN, --S(CH₂)_(t) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), or --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸ ;

R¹⁴ is --H;

R¹⁸ and R¹⁹ are independently

H, halo (F, Cl, Br, I), C₁ -C₆ -alkyl, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(t) CN, --NH(CH₂)_(t) CN, --S(CH₂)_(t) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -phenyl), or --O(C═O)phenyl;

R18 and R19 can be taken together to form a methylenedioxy group;

R²⁰ is selected from the group consisting of:

(CH₂)_(r) --D, or --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸ ;

and all other required substituents of formula (I) are defined as in claim 3.

Specifically preferred are those most preferred compounds listed below:

N¹ -(4-phenylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(3-phenoxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(1-fluorenonyl)-(R)-boroarginine, hydrochloride

N¹ -(4-[1-butyl]benzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-benzoylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(5-phenyl-2-furoyl)-(R)-boroarginine, hydrochloride

N¹ -(3-[N-benzyloxycarbonyl-N-methylamino]-4-[1-butyl]benzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-phenyl-4-isoquinoloyl)-(R)-boroarginine, hydrochloride

N¹ -(4-cyclohexylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -[4-phenyl-2-nitrobenzoyl]boroArg, (+)-pinanediol ester

N¹ -[4-phenyl-2-fluorobenzoyl]boroArg, (+)-pinanediol ester

N¹ -[4-phenyl-2-aminobenzoyl]boroArg, (+)-pinanediol ester

N¹ -[4-phenyl-2-(methylsulfonamido)benzoyl]boroArg, (+)-pinanediol ester

N¹ -[4-phenyl-2-(cyanomethylamino)benzoyl]boroArg, (+)-pinanediol ester

N¹ -[4-phenyl-2-(cyanomethyl)benzoyl]boroArg, (+)-pinanediol ester

N¹ -[4-phenyl-2-(diethylamino)benzoyl]boroArg, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg, (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg, (+)pinanediol ester

N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]benzoyl]boroArg, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]benzoyl]boroArg-OH

N¹ -[4-[2-(n-butoxycarbonylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg, (+)-pinanediol ester

N¹ -[4-[2-(diethylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg, (+)pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-fluorobenzoyl]boroArg, (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-fluorobenzoyl]boroArg, (+)pinanediol ester

N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-fluorobenzoyl]boroArg, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-nitrobenzoyl]boroArg, (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-nitro-benzoyl]boroArg, (+)pinanediol ester

N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-nitrobenzoyl]boroArg, (+)-pinanediol ester

N¹ -(3-phenylbenzoyl)boroArg, (+)-pinanediol

N¹ -[4-(3-BOCNHphenyl)2-methyl-benzoyl]boroarg, (+)-pinanediol

N¹ -(5-phenyl-2-furoyl)boroarg, (+)-pinanediol

N¹ -(5-phenyl -2-thienyl)boroarg, (+)-pinanediol

N¹ -[4-(3-nitrophenyl)benzoyl]boroarg, (+)-pinanediol

N¹ -[4-(3-aminophenyl)benzoyl]boroarg, (+)-pinanediol

N¹ -(3-phenylbenzoyl)borolys, (+)-pinanediol

N¹ -(5-phenyl-2-furoyl)boroarg-OH

N¹ -3-phenylbenzoyl)boroIrg, (+)-pinanediol

(R)-[5-amino-1-[[[5-(phenylmethyl)-1H-1,2,4-triazol-1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride

[3aS-[2(S*),3aα,4β,6β]]-(1,1-dimethylethyl) [3-[5-[[[4-[(amino-iminomethyl)amino]-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzo-dioxaborol-2-yl)butyl]amino]carbonyl]-2-thienyl]phenyl]carbamate hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-5-(phenyl-methyl)-3-(2H-tetrazol-5-ylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-1-[2-[[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]amino]-2-oxoethyl]-5-(phenylmethyl)-1H-1,2,4-triazole-3-acetic acid hydrochloride 1:1 with [3aS-[2(S*),3aα,4β,6β,7aα]]-1-[2-[[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]amino]-2-oxoethyl]-3-(phenylmethyl)-1H-1,2,4-triazole-5-acetic acid hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-methyl 1-[2-[[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-amino]-2-oxoethyl]-5-(phenylmethyl)-1H-1,2,4-triazole-3-acetate hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-methyl 1-[2-[[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-amino]-2-oxoethyl]-3-(phenylmethyl)-1H-1,2,4-triazole-5-acetate hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3-phenyl-5-(phenyl-methyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

(R)-[5-amino-1-[[[3-phenyl-5-(phenylmethyl)-1H-1,2,4-triazol-1-yl]acetyl]-amino]pentyl]boronic acid hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3-(3-nitro-phenyl)-5-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[4-[(aminoiminomethyl)amino]-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) butyl]-3-(3-nitrophenyl)-5-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3,5-bis(phenyl-methyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[4-[(aminoiminomethyl)amino]-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)butyl]-3,5-bis(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide

(R)-[5-amino-1-[[[3-(phenylmethyl)-1H-2,2,4-triazol-1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-5-methyl-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

[3aS-[2(R*),3aα,4β,6β]]-N-[5-amino-1-(hexahydro-3a,5,5-tri-methyl-4,6-methano-1,3,2-benzodioxaborol-2-yl pentyl]-5-[(phenyl-methoxy)methyl]-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-5-(cyanomethyl)-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3-(phenylmethyl)-5-propyl-1H-1,2,4-triazole-1-acetamide hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-5-phenyl-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

(R)-[5-amino-1-[[[5-methyl-3-(phenylmethyl)-1H-1,2,4-triazol-1-yl]acetyl]-amino]pentyl]boronic acid hydrochloride

[2aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3-phenyl-1H-1,2,4-triazole-1-acetamide hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-5-methyl-3-phenyl-1H-1,2,4-triazole-1-acetamide hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-5-(2-phenyl-ethyl)-1H-1,2,4-triazole-1-acetamide

(R)-[5-amino-1-[[[5-(2-phenylethyl)-1H-1,2,4-triazol-1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3,5-bis(2-phenyl-ethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride

(R)-[5-amino-1-[[[3,5-bis(2-phenylethyl)-1H-1,2,4-triazol-1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3-(2-phenylethyl)-1H-1,2,4-triazole-1-acetamide

(R)-[5-amino-1-[[[3-(2-phenylethyl)-1H-1,2,4-triazol-1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3-(3-phenyl-propyl)-1H-1,2,4-triazole-1-acetamide

(R)-[5-amino-1-[[[5-(3-phenylpropyl)-1H-1,2,4-triazol-1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride

(R)-[5-amino-1-[[[3-(3-phenylpropyl)-1H-1,2,4-triazol-1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-1,5-bis(phenyl-methyl)-1H-1,2,4-triazole-3-acetamide hydrochloride 2:8 with (R)-[5-amino-1-[[[1,5-bis(phenylmethyl)-1H-1,2,4-triazol-3-yl]acetyl]amino]-pentyl]boronic acid hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-4-methyl-2-phenyl-5-pyrimidinecarboxamide hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-2,4-diphenyl-5-pyrimidinecarboxamide hydrochloride

[3aS-[2(S*),3aα,4β,6β,7aα]]-N-[4-[(amimoiminomethyl)amino]-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)butyl]-4-methyl-2-phenyl-5-pyrimidinecarboxamide hydrochloride

[3aS-[2(S*),3α,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-6-phenyl-3-pyrimidinecarboxamide hydrochloride

(R)-[5-amino-1-[[(6-phenyl-3-pyridinyl)carbonyl]amino]pentyl]boronic acid dihydrochloride

Illustrative of the compounds of this invention are the following:

N¹ -(4-phenylbenzoyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(3-phenylbenzoyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(3-phenoxybenzoyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(4-[4-pyridyl]benzoyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(2-benzoylbenzoyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(3-benzoylbenzoyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(4-benzoylbenzoyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(3-[N-benzyloxycarbonyl]aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(3-[N-benzyloxycarbonyl-N-methyl]aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-ethylbenzoyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(4-n-propylbenzoyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(4-isopropylbenzoyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(4-n-butylbenzoyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(4-tert-butylbenzoyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(4-n-hexylbenzoyl)-(R)-boroarginine(+)-pinanediol, bisulfite

N¹ -(4-cyclohexylbenzoyl)-(R)-boroarginine(+)pinanediol, bisulfite

N¹ -(2-[N-(2-phenylethyl)carbonyl]aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-n-butyloxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-[N-cyclopropylcarbonyl]aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-[N-cyclohexylcarbonyl]aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-[N-(4-methoxy)benzoyl]aminobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-[4-methoxy]phenylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-[2-phenyl]benzyloxycarbonylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-[1-naphthyl]benzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-[4-carboxy]phenylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(4-phenylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3-phenylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3-phenoxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-benzoylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3-benzoylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-benzoylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3-[N-benzyloxycarbonyl]aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3-[N-benzyloxycarbonyl-N-methyl]aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-ethylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-n-propylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-isopropylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-n-butylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-tert-butylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-n-hexylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-cyclohexylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-[N-(2-phenylethyl)carbonyl]aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-n-butyloxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-[N-cyclopropylcarbonyl]aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-[N-cyclohexylcarbonyl]aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-[N-(4-methoxy)benzoyl]aminobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-[4-methoxy]phenylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-[2-phenyl]benzyloxycarbonyl]benzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-[1-naphthyl]benzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-[4-carboxy]phenylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -([2-anthraquinonyl]carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -([2-dioxothioxanthinonyl]carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -([2-anthraquinonyl]carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -([2-dioxothioxanthinonyl]carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -([2-fluoren-9-onyl]carbonyl)-(R)-borothiohomoarginine (+)-pinanediol, hydrobromide

N¹ -([2-fluoren-9-onyl]carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -([2-fluoren-9-onyl]carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -([3-fluoren-9-onyl]carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -([3-fluoren-9-onyl]carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -([4-fluoren-9-onyl]carbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -([4-fluoren-9-onyl]carbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(1-naphthoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(1-naphthoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-phenyl-5-trifluoromethyl-benzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-methoxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-carboxamidobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-fluorobenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-trifluoromethylbenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-chlorobenzoyl )-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-hydroxybenzoyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-methoxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-carboxamidobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-fluorobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-trifluoromethylbenzoyl)-(R)-boroarginine (+) pinanediol, bisulfite

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-chlorobenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-hydroxybenzoyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-[5-phenyl]furylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-[5-phenyl]thiophen-ylcarbonyl )-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-[5-phenyl]furylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-[5-phenyl]thiophen-ylcarbonyl )-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3-[6-phenyl]pyridylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(3-[5-benzyloxy]pyridylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(3-[6-phenyl]pyridylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3-[5-benzyloxy]pyridylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-benzopyronylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-benzopyronylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(3-isoquinolinylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(3-isoquinolinylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-phenyl-4-isoquinolinylcarbonyl )-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(2-isoquinolinylcarbonyl)-(R)-boroarginine (+)-pinanediol, bisulfite

N¹ -(2-isoquinolinylcarbonyl)-(R)-borothioarginine (+)-pinanediol, hydrobromide

N¹ -(4-phenylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(3-phenylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(3-phenoxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-[4-pyridyl]benzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-benzoylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(3-benzoylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-benzoylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(3-[N-benzyloxycarbonyl]aminobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(3-[N-benzyloxycarbonyl-N-methyl]aminobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-ethylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-n-propylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-isopropylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-tert-butylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-n-hexylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-cyclohexylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-[N-(2-phenylethyl)carbonyl]aminobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-n-butyloxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-[N-cyclopropylcarbonyl]aminobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-[N-cyclohexylcarbonyl]aminobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-[N-(4-methoxy)benzoyl]aminobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-[4-methoxy]phenylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-[2-phenyl]benzyloxycarbonylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-[1-naphthyl]benzoyl)-(R)-boroarginine, hydrochloride

N¹ -(4-[4-carboxy]phenylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -([2-anthraquinonyl]carbonyl)-(R)-boroarginine, hydrochloride

N¹ -([2-dioxothioxanthinonyl]carbonyl)-(R)-boroarginine, hydrochloride

N¹ -([2-fluoren-9-onyl]carbonyl)-(R)-boroarginine, hydrochloride

N¹ -([3-fluoren-9-onyl]carbonyl)-(R)-boroarginine, hydrochloride

N¹ -(1-naphthoyl)-(R)-boroarginine, hydrochloride

N¹ -([4-fluoren-9-onyl]carbonyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-methoxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-carboxamidobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-fluorobenzoyl )-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-trifluoromethylbenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-chlorobenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-hydroxybenzoyl)-(R)-boroarginine, hydrochloride

N¹ -(2-[5-phenyl]furylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(2-[5-phenyl]thiophen-ylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(2-benzopyronylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(2-isoquinolinylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(3-isoquinolinylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(4-phenylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(3-phenylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(3-phenoxybenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-benzoylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(3-benzoylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-benzoylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(3-[N-benzyloxycarbonyl]aminobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(3-[N-benzyloxycarbonyl-N-methyl]aminobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-ethylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-n-propylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-isopropylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-n-butylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-tert-butylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-n-hexylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-cyclohexylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-[N-(2-phenylethyl)carbonyl]aminobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-n-butyloxybenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-[N-cyclopropylcarbonyl]aminobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-[N-cyclohexylcarbonyl]aminobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-[N-(4-methoxy)benzoyl]aminobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-[4-methoxy]phenylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-[2-phenylbenzyloxycarbonyl]benzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-[1-naphthyl]benzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-[4-carboxy]phenylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -([2-anthraquinonyl]carbonyl)-(R)-borothioarginine, hydrochloride

N¹ -([2-dioxothioxanthinonyl]carbonyl)-(R)-borothioarginine, hydrochloride

N¹ -([2-fluoren-9-onyl]carbonyl)-(R)-borothiohomoarginine, hydrochloride

N¹ -([2-fluoren-9-onyl]carbonyl)-(R)-borothioarginine, hydrochloride

N¹ -([3-fluoren-9-onyl]carbonyl)-(R)-borothioarginine, hydrochloride

N¹ -([4-fluoren-9-onyl]carbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(1-naphthoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R) borothioarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-methoxybenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-carboxamidobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-fluorobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-trifluoromethylbenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-chlorobenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-hydroxybenzoyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-[5-phenyl]furylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-[5-phenyl]thiophenylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(3-[6-phenyl]pyridylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(3-[5-benzyloxy]pyridylcarbonyl)-(R)-boroarginine, hydrochloride

N¹ -(3-[6-phenyl]pyridylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(3-[5-benzyloxy]pyridylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-benzopyronylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(3-isoquinolinylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(2-isoquinolinylcarbonyl)-(R)-borothioarginine, hydrochloride

N¹ -(4-phenylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(3-phenylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(3-phenoxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-[4-pyridyl]benzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-benzoylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(3-benzoylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-benzoylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(3-[N-benzyloxycarbonyl]aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(3-[N-benzyloxycarbonyl-N-methyl]aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-ethylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-n-propylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-isopropylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-tert-butylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-n-hexylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-cyclohexylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-[N-(2-phenylethyl)carbonyl]aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-n-butyloxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-[N-cyclopropylcarbonyl]aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-[N-cyclohexylcarbonyl]aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-[N-(4-methoxy)benzoyl]aminobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-[4-methoxy]phenylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-[2-phenyl]benzyloxycarbonylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-[1-naphthyl]benzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-[4-carboxy]phenylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -([2-anthraquinonyl]carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -([2-dioxothioxanthinonyl]carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -([2-fluoren-9-onyl]carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -([3-fluoren-9-onyl]carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(1-naphthoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -([4-fluoren-9-onyl]carbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-methoxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4 -[4-carboxy]phenyl-5-carboxamidobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-fluorobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-trifluoromethylbenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-chlorobenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-hydroxybenzoyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-[5-phenyl]furylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-[5-phenyl]thiophen-ylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-benzopyronylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-isoquinolinylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(3-isoquinolinylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-borolysine (+)-pinanediol, hydrochloride

N¹ -(4-phenylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(3-phenylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(3-phenoxybenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-[4-pyridyl]benzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-benzoylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(3-benzoylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-benzoylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(3-[N-benzyloxycarbonyl]aminobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(3-[N-benzyloxycarbonyl-N-methyl]aminobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-ethylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-n-propylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-isopropylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-tert-butylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-n-hexylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-cyclohexylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-[N-(2-phenylethyl)carbonyl]aminobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-n-butyloxybenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-[N-cyclopropylcarbonyl]aminobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-[N-cyclohexylcarbonyl]aminobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-[N-(4-methoxy)benzoyl]aminobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-[4-methoxy]phenylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-[2-phenyl]benzyloxycarbonylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-[1-naphthyl]benzoyl)-(R)-borolysine, hydrochloride

N¹ -(4-[4-carboxy]phenylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -([2-anthraquinonyl]carbonyl)-(R)-borolysine, hydrochloride

N¹ -([2-dioxothioxanthinonyl]carbonyl)-(R)-borolysine, hydrochloride

N¹ -([2-fluoren-9-onyl]carbonyl)-(R)-borolysine, hydrochloride

N¹ -([3-fluoren-9-onyl]carbonyl)-(R)-borolysine, hydrochloride

N¹ -(1-naphthoyl)-(R)-borolysine, hydrochloride

N¹ -([4-fluoren-9-onyl]carbonyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-methoxybenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-carboxamidobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-fluorobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-trifluoromethylbenzoyl)-(R) borolysine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-chlorobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-phenyl-5-hydroxybenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-methoxybenzoyl)-(R)-borolysine, hydrochloride

N² -(2-methyl-4-[4-carboxy]phenyl-5-carboxamidobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-fluorobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-trifluoromethylbenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-chlorobenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-[4-carboxy]phenyl-5-hydroxybenzoyl)-(R)-borolysine, hydrochloride

N¹ -(2-[5-phenyl]furylcarbonyl)-(R)-borolysine, hydrochloride

N¹ -(2-[5-phenyl]thiophenylcarbonyl)-(R)-borolysine, hydrochloride

N¹ -(2-benzopyronylcarbonyl)-(R)-borolysine, hydrochloride

N¹ -(2-isoquinolinylcarbonyl)-(R)-borolysine, hydrochloride

N¹ -(3-isoquinolinylcarbonyl)-(R)-borolysine, hydrochloride

N¹ -(2-phenyl-4-isoquinolinylcarbonyl)-(R)-borolysine, hydrochloride

N¹ -(2-methyl-4-phenylbenzoyl)-R-borolysine, hydrochloride

N¹ -(2-methyl-4-phenylbenzoyl)-R-borolysine, (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenylbenzoyl)-R-borothioarginine, hydrobromide

N¹ -(2-methyl-4-phenylbenzoyl)-R-borothioarginine, (+)-pinanediol, hydrochloride

N¹ -(2-methyl-4-phenylbenzoyl)-R-boroarginine, hydrochloride

N¹ -(2-methyl-4-phenylbenzoyl)-R-boroarginine, (+)-pinanediol, bisulfite

N¹ -[4-phenyl-2-nitrobenzoyl]boroArg(Me), (+)-pinanediol ester

N¹ -[4-phenyl-2-fluorobenzoyl]boroArg(Me),(+)-pinanediol ester

N¹ -[4-phenyl-2-aminobenzoyl]boroArg(Me), (+)-pinanediol ester

N¹ -[4-phenyl-2-(methylsulfonamido)benzoyl]boroArg(Me), (+)-pinanediol ester

N¹ -[4-phenyl-2-(cyanomethylamino)benzoyl]boroArg(Me), (+)-pinanediol ester

N¹ -[4-phenyl-2-(cyanomethyl)benzoyl]boroArg(Me), (+)-pinanediol ester

N¹ -[4-phenyl-2-(diethylamino)benzoyl]boroArg(Me), (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-methylbenzoyl]boroArg(Me), (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg(Me), (+)pinanediol ester

N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg(Me), (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]benzoyl]boroArg(Me), (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl) phenyl]benzoyl]boroArg(Me)-OH

N¹ -[4-[2-(n-butoxycarbonylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg(Me), (+)-pinanediol ester

N¹ -[4-[2-(diethylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg(Me), (+)pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-fluorobenzoyl]boroArg(Me), (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-fluorobenzoyl]boroArg(Me), (+)pinanediol ester

N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-fluorobenzoyl]boroArg(Me), (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-nitrobenzoyl]boroArg(Me), (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-nitrobenzoyl]boroArg(Me), (+)pinanediol ester

N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-nitrobenzoyl]boroArg(Me), (+)-pinanediol ester.

N¹ -[4-phenyl-2-nitrobenzoyl]boroMPG, (+)-pinanediol ester

N¹ -[4-phenyl-2-fluorobenzoyl]boroMPG, (+)-pinanediol ester

N¹ -[4-phenyl-2-aminobenzoyl]boroMPG, (+)-pinanediol ester

N¹ -[4-phenyl-2-(methylsulfonamido)benzoyl]boroMPG, (+)-pinanediol ester

N¹ -[4-phenyl-2-(cyanomethylamino)benzoyl]boroMPG, (+)-pinanediol ester

N¹ -[4-phenyl-2-(cyanomethyl)benzoyl]boroMPG, (+)-pinanediol ester

N¹ -[4-phenyl-2-(diethylamino)benzoyl]boroMPG, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroMPG, (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-methyl-benzoyl]boroMPG, (+)pinanediol ester

N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroMPG, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]benzoyl]boroMPG, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]benzoyl]boroMPG-OH

N¹ -[4-[2-(n-butoxycarbonylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroMPG, (+)-pinanediol ester

N¹ -[4-[2-(diethylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroMPG, (+)pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-fluorobenzoyl]boroMPG, (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-fluorobenzoyl]boroMPG, (+)pinanediol ester

N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-fluorobenzoyl]boroMPG, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-nitrobenzoyl]boroMPG, (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-nitro-benzoyl]boroMPG, (+)pinanediol ester

N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-nitrobenzoyl]boroMPG, (+)-pinanediol ester.

N¹ -[4-phenyl-2-nitrobenzoyl]boroACA, (+)-pinanediol ester

N¹ -[4-phenyl-2-fluorobenzoyl]boroACA, (+)-pinanediol ester

N¹ -[4-phenyl-2-aminobenzoyl]boroACA, (+)-pinanediol ester

N¹ -[4-phenyl-2-(methylsulfonamido)benzoyl]boroACA, (+)-pinanediol ester

N¹ -[4-phenyl-2-(cyanomethylamino)benzoyl]boroACA, (+)-pinanediol ester

N¹ -[4-phenyl-2-(cyanomethyl)benzoyl]boroACA, (+)-pinanediol ester

N¹ -[4-phenyl-2-(diethylamino)benzoyl]boroACA, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroACA, (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-methyl-benzoyl]boroACA, (+)pinanediol ester

¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroACA, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]benzoyl]boroACA, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]benzoyl]boroACA-OH

N¹ -[4-[2-(n-butoxycarbonylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroACA, (+)-pinanediol ester

N¹ -[4-[2-(diethylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroACA, (+)pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-fluorobenzoyl]boroACA, (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-fluorobenzoyl]boroACA, (+)pinanediol ester

N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-fluorobenzoyl]boroACA, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-nitrobenzoyl]boroACA, (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-nitro-benzoyl]boroACA, (+)pinanediol ester

N¹ -[2-(methoxycarbonylaminosulfonyl)phenyl]-2-nitro-benzoyl]boroACA, (+)-pinanediol ester

N¹ -[4-phenyl-2-nitrobenzoyl]boroLys, (+)-pinanediol ester

N¹ -[4-phenyl-2-fluorobenzoyl]boroLys, (+)-pinanediol ester

N¹ -[4-phenyl-2-aminobenzoyl]boroLys, (+)-pinanediol ester

N¹ -[4-phenyl-2-(methylsulfonamido)benzoyl]boroLys, (+)-pinanediol ester

N¹ -[4-phenyl-2-(cyanomethylamino)benzoyl]boroLys, (+)-pinanediol ester

N¹ -[4-phenyl-2-(cyanomethyl)benzoyl]boroLys, (+)-pinanediol ester

N¹ -[4-phenyl-2-(diethylamino)benzoyl]boroLys, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroLys, (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-methyl-benzoyl]boroLys, (+)-pinanediol ester

N¹ -[4-[2-(methoxycabonylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroLys, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]benzoyl]boroLys, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]benzoyl]boroLys-OH

N¹ -[4-[2-(n-butoxycarbonylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroLys, (+)-pinanediol ester

N¹ -[4-[2-(diethylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroLys, (+)pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-fluorobenzoyl]boroLys, (+)pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-fluorobenzoyl]boroLys, (+)pinanediol ester

N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-fluorobenzoyl]boroLys, (+)-pinanediol ester

N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-nitrobenzoyl]boroLys, (+) pinanediol ester

N¹ -[4-[2-(aminosulfonyl)phenyl]-2-nitro-benzoyl]boroLys, (+)pinanediol ester

N¹ -[4-[2-(methoxyaminosulfonyl)phenyl]-2-nitrobenzoyl]boroLys, (+)-pinanediol ester.

DETAILED DESCRIPTION OF THE INVENTION

Throughout the specification, the following conventional three-letter abbreviations for amino acid residues or amino acids apply:

Ala=alanine

Arg=arginine

Asn=asparagine

Asp=aspartic acid

Cys=cysteine

Gln=glutamine

Glu=glutamic acid

Gly=glycine

His=histidine

Ile=isoleucine

Leu=leucine

Lys=lysine

Met=methionine

Phe=phenylalanine

Pro=proline

Ser=serine

Thr=threonine

Trp=tryptophan

Tyr=tyrosine

Val=valine

Irg=arginine where the guanidine is replaced with an isothiouronium (--SC(═NH)NH₂)

Arg(Me)=arginine with the guanidino group methylated

MPG=5-methoxy-propylglycine

ACA=3-(4-amino)cyclohexylalanine

The prefix "boro" indicates amino acid residues where the carboxy group is replaced by a boronic acid (Formula I, Y¹ and Y² =--OH).

The pinanediol boronic acid ester and the pinacol boronic acid ester are abbreviated "--C₁₀ H₁₆ --" and --C₆ H₁₂ --" respectively. Other illustrations of diols useful for deriving a boronic acid orthoesters are 1,2-ethanediol, 1,3-propanediol, 1,2-propanediol, 2,3-butanediol, 1,2-diisopropylethanediol, 5,6-decanediol, 1,2-dicyclohexylethanediol.

The formamidino modified amino group is abbreviated (CH═NH). For example, the formamidino analog of -boroOrn--OH {--NH--CH[(CH₂)₃ --NH--CH(NH)H]B(OH)₂ } is -boroOrn(CH═NH)--OH. Analogs containing sidechain substituents are described by indicating the substituent in parenthesis following the name of the parent residue. For example the analog of boroPhenylalanine containing a meta cyano group is -boroPhe(mCN)--. N-alkyl substituents on the guanidino group of boroArg- or on the isothiouronium analogs (boroIrg) are also put in parenthesis in a similar manner.

Other abbreviations are: Z, benzyloxycarbonyl; BSA, benzene sulfonic acid; THF, tetrahydrofuran; Boc-, t-butoxycarbonyl-; Ac-, acetyl; pNA, p-nitro-aniline; DMAP, 4-N,N-dimethylaminopyridine; Tris, Tris(hydroxymethyl)aminomethane; MS, mass spectrometry; FAB/MS, fast atom bombardment mass spectrometry. LRMS(NH₃ --CI) and HRMS(NH₃ --CI) are low and high resolution mass spectrometry, respectively, using NH₃ as an ion source.

As used herein, the structure ##STR30## wherein J is N or C and K, L, M and Q are independently selected at each occurrence from the group consisting of N, CR¹³, S or O, provided that:

i) there may be only one S or O present in the ring at a time;

ii) there may only be 1-2N present when there is an O or S present;

iii) there may be only 1-4N present;

is used as a substituent definition for R¹. This substituent may be exemplified by the following structures where --J--K--L--M--Q-- is:

1) --N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,

2) --N--C(R¹³)═C(R¹³)--C(R¹³)═N--,

3) --N--C(R¹³)═C(R¹³)--N═C(R¹³)--,

4) --N--C(R¹³)═N--C(R¹³)═N--,

5) --N--C(R¹³)═C(R¹³)--N═N--

6) --N--C(R¹³)═N--N═N--,

7) --N--N═C(R¹³)--N═N--,

8) ═C--O--C(R¹³)═N--C(R¹³)═,

9) --C═C(R¹³)--O--C(R¹³)═N--,

10) ═C--O--C(R¹³)═C(R¹³)--N═,

11) --C═C(R¹³)--C(R¹³)═N--O--,

12) ═C--C(R¹³)═C(R¹³)--O--N═,

13) --C═C(R¹³)--O--N═C(R¹³)--,

14) ═C--S--C(R¹³)═N--C(R¹³)═,

15) --C═C(R¹³)--S--C(R¹³)═N--,

16) ═C--S--C(R¹³)═C(R¹³)--N═,

17) --C═N--S--N═C(R¹³)--,

18) --C═N--S--C(R¹³)═N--,

19) ═C--S--N═C(R¹³)--N═,

20) ═C--S--C(R¹³)═C(R¹³)--C(R¹³)═,

21) --C═C(R¹³)--S--C(R¹³)═C(R¹³)--,

22) ═C--O--C(R¹³)═C(R¹³)--C(R¹³)═, or

23) --C═C(R¹³)--O--(R¹³)═C(R¹³)--.

As used herein, the structure ##STR31## wherein in W, R, T, U and V are independently selected at each occurrence from the group consisting of: CR¹³ or N, provided that there may be only 1-3N present, is used as a substituent definition for R¹. This substituent may be exemplified by the following structures where --C--W--R--T--U--V-- is:

1) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,

2) --C═C(R¹³)--N═C(R¹³)--C(R¹³)═C(R¹³)--,

3) --C═C(R¹³)--C(R¹³)═N--C(R¹³)═C(R¹³)--,

4) --C═N--N═C(R¹³)--C(R¹³)═C(R¹³)--,

5) --C═C(R¹³)--N═N--C(R¹³)═C(R¹³)--,

6) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═N--,

7) --C═N--C(R¹³)═C(R¹³)--N═C(R¹³)--,

8) --C═N--C(R¹³)═N--C(R¹³)═C(R¹³)--,

9) --C═C(R¹³)--N═C(R¹³)--N═C(R¹³)--,

10) --C═N--C(R¹³)═N--N═C(R¹³)--,

11) --C═N--C(R¹³)═C(R¹³)--N═N--, or

12) --C═C(R¹³)--N═C(R¹³)--N═N--.

"Amino acid residues" as used herein, refers to natural or unnatural amino acids of either D- or L-configuration. Natural amino acids residues are Ala, Arg, Asn, Asp, Aze, Cys, Gln, Glu, Gly, His, Ile, Irg Leu, Lys, Met, Orn, Phe, Phe(4-fluoro), Pro, Sar, Ser, Thr, Trp, Tyr, and Val. Roberts and Vellaccio, The Peptides, Vol 5; 341-449 (1983), Academic Press, New York, discloses numerous suitable unnatural amino acids and is incorporated herein by reference for that purpose.

"Amino acids residues" also refers to various amino acids where sidechain functional groups are coupled with appropriate protecting groups known to those skilled in the art. "The Peptides", Vol 3, 3-88 (1981) discloses numerous suitable protecting groups and is incorporated herein by reference for that purpose.

The reactions of the synthetic methods claimed herein are carried out in suitable solvents which may be readily selected by one of skill in the art of organic synthesis, said suitable solvents generally being any solvent which is substantially nonreactive with the starting materials (reactants), the intermediates, or products at the temperatures at which the reactions are carried out, i.e., temperatures which may range from the solvent's freezing temperature to the solvent's boiling temperature. A given reaction may be carried out in one solvent or a mixture of more than one solvent. Depending on the particular reaction step, suitable solvents for a particular reaction step may be selected.

The compounds herein described may have asymmetric centers. All chiral, diastereomeric, and racemic forms are included in the present invention. Many geometric isomers of olefins, C═N double bonds, and the like can also be present in the compounds described herein, and all such stable isomers are contemplated in the present invention. It will be appreciated that certain compounds of the present invention contain an asymmetrically substituted carbon atom, and may be isolated in optically active or racemic forms. It is well known in the art how to prepare optically active forms, such as by resolution of racemic forms or by synthesis, from optically active starting materials. Also, it is realized that cis and trans geometric isomers of the compounds of the present invention are described and may be isolated as a mixture of isomers or as separated isomeric forms. All chiral, diastereomeric, racemic forms and all geometric isomeric forms of a structure are intended, unless the specific stereochemistry or isomer form is specifically indicated.

When any variable (for example, R¹ through R²⁰, R^(20a), m, n, D, E, F, W, X, etc.) occurs more than one time in any constituent or in Formula (I), its definition on each occurrence is independent of its definition at every other occurrence. Thus, for example, if a group is shown to be substituted with 0-3 R¹¹, then said group may optionally be substituted with up to three R¹¹ and R¹¹ at each occurrence is selected independently from the defined list of possible R¹¹. Also, for example, in --N(R¹⁵)₂, each of the R¹⁵ substituents may be independently selected from the list of possible R²⁰ groups defined. Also, combinations of substituents and/or variables are permissible only if such combinations result in stable compounds. Similarly, by way of example, for the group --C(R¹¹)₂ --, each of the two R¹¹ substituents on C is independently selected from the defined list of possible R¹¹.

As used herein, "alkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms; "haloalkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms, substituted with 1 or more halogen (for example --C_(v) F_(w) where v=1 to 3 and w=1 to (2v+1)); "alkoxy" represents an alkyl group of indicated number of carbon atoms attached through an oxygen bridge; "cycloalkyl" is intended to include saturated ring groups, including mono-,bi- or poly-cyclic ring systems, such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, adamantyl and cyclooctyl; and "biycloalkyl" is intended to include saturated bicyclic ring groups such as [3.3.0]bicyclooctane, [4.3.0]bicyclononane, [4.4.0]bicyclodecane (decalin), [2.2.2]bicyclooctane, and so forth. "Alkenyl" is intended to include hydrocarbon chains of either a straight or branched configuration and one or more unsaturated carbon-carbon bonds which may occur in any stable point along the chain, such as ethenyl, propenyl, and the like; and "alkynyl" is intended to include hydrocarbon chains of either a straight or branched configuration and one or more triple carbon-carbon bonds which may occur in any stable point along the chain, such as ethynyl, propynyl and the like.

"Halo" or "halogen" as used herein refers to fluoro, chloro, bromo, and iodo; and "counterion" is used to represent a small, negatively charged species such as chloride, bromide, hydroxide, acetate, sulfate, and the like.

As used herein, "aryl" or "aromatic residue" is intended to mean phenyl or naphthyl; the term "arylalkyl" represents an aryl group attached through an alkyl bridge. By way of examples: the term "C₇ -C₁₀ arylalkyl" is intended to refer to an aryl group attached through a C₁ -C₄ alkyl bridge to the residue of the indicated compound; the term "(C₁ -C₃ alkyl)aryl" is intended to refer to a C₁ -C₃ alkyl group which is attached through an aryl ring to the residue of the indicated compound; the term "aryl(C₁ -C₃ alkyl)" is intended to refer to an aryl group attached through a C₁ -C₃ alkyl group to the residue of the indicated compound.

As used herein, "carbocycle" or "carbocyclic residue" is intended to mean any stable 3- to 8-membered monocyclic or bicyclic or 7- to 14-membered bicyclic or tricyclic or an up to 26-membered polycyclic carbon ring, any of which may be saturated, partially unsaturated, or aromatic. Examples of such carbocyles include, but are not limited to, cyclopropyl, cyclopentyl, cyclohexyl, phenyl, biphenyl, naphthyl, indanyl, adamantyl, or tetrahydronaphthyl (tetralin).

As used herein, the term "heterocycle" is intended to mean a stable 5- to 7- membered monocyclic or bicyclic or 7- to 10-membered bicyclic heterocyclic ring which is saturated and consists of carbon atoms and from 1 to 4 heteroatoms independently selected from the group consisting of N, O and S and wherein the nitrogen and sulfur heteroatoms may optionally be oxidized, and the nitrogen may optionally be quaternized, and including any bicyclic group in which any of the above-defined heterocyclic rings is fused to a benzene ring. The heterocyclic ring may be attached to its pendant group at any heteroatom or carbon atom which results in a stable structure. The term "heteroaryl" is intended to mean an aromatic form of a heterocyclic ring. Unless otherwise specified, the heterocyclic and heteroaryl rings described herein may be substituted on carbon or on a nitrogen atom if the resulting compound is stable. Unless otherwise specified, examples of such heterocycles include, but are not limited to, pyridinyl, pyrimidinyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, tetrazolyl, benzofuranyl, benzothiophenyl, indolyl, indolenyl, quinolinyl, isoquinolinyl, benzimidazolyl, piperidinyl, 4-piperidonyl, pyrrolidinyl, 2-pyrrolidonyl, pyrrolinyl, tetrahydrofuranyl, tetrahydroquinolinyl, tetrahydroisoquinolinyl, decahydroquinolinyl or octahydroisoquinolinyl, azocinyl, triazinyl, 6H-1,2,5-thiadiazinyl, 2H, 6H-1,5,2-dithiazinyl, thiophenyl, thianthrenyl, pyranyl, isobenzofuranyl, chromenyl, xanthenyl, phenoxathiinyl, 2H-pyrrolyl, isothiazolyl, isoxazolyl, pyrazinyl, pyridazinyl, indolizinyl, isoindolyl, 3H-indolyl, 1H-indazolyl, purinyl, 4H-quinolizinyl, phthalazinyl, naphthyridinyl, quinoxalinyl, quinazolinyl, cinnolinyl, pteridinyl, 4aH-carbazolyl, carbazolyl, β-carbolinyl, phenanthridinyl, acridinyl, perimidinyl, phenanthrolinyl, phenazinyl, phenarsazinyl, phenothiazinyl, furazanyl, phenoxazinyl, isochromanyl, chromanyl, imidazolidinyl, imidazolinyl, pyrazolidinyl, pyrazolinyl, piperazinyl, indolinyl, isoindolinyl, quinuclidinyl, morpholinyl, oxazolidinyl, benzotriazolyl, benzisoxazolyl, oxindolyl, benzoxazolinyl, or isatinoyl. Also included are fused ring and spiro compounds containing, for example, the above heterocycles.

When a bond to a substituent is shown to cross the bond connecting two atoms in a ring, then such substituent may be bonded to any atom on the ring. When a substituent is listed without indicating the atom via which such substituent is bonded to the rest of the compound of formula I, then such substituent may be bonded via any atom in such substituent. For example, when the substituent is piperazinyl, piperidinyl, or tetrazolyl, unless specified otherwise, said piperazinyl, piperidinyl, tetrazolyl group may be bonded to the rest of the compound of formula (I) via any atom in such piperazinyl, piperidinyl, tetrazolyl group.

Combinations of substituents and/or variables are permissible only if such combinations result in stable compounds. By stable compound or stable structure it is meant herein a compound that is sufficiently robust to survive isolation to a useful degree of purity from a reaction mixture, and formulation into an efficacious therapeutic agent.

The term "substituted", as used herein, means that an one or more hydrogen on the designated atom is replaced with a selection from the indicated group, provided that the designated atom's normal valency is not exceeded, and that the substitution results in a stable compound. When a substituent is keto (i.e., ═O), then 2 hydrogens on the atom are replaced.

As used herein, the term "any group that, when administered to a mammalian subject, cleaves to form a free hydroxyl, amino or sulfhydryl" means any group bonded to an O, N, or S atom, respectively, which is cleaved from the O, N, or S atom when the compound is administered to a mammalian subject to provide a compound having a remaining free hydroxyl, amino, or sulfhydryl group, respectively. Examples of groups that, when administered to a mammalian subject, are cleaved to form a free hydroxyl, amino or sulfhydryl, include but are not limited to, phosphate esters, C₁ -C₆ alkyl substituted with 0-3R¹¹, C₃ -C₆ alkoxyalkyl substituted with 0-3R¹¹, C₁ -C₆ alkylcarbonyl substituted with 0-3R¹¹, C₁ -C₆ alkoxycarbonyl substituted with 0-3R¹¹, C₁ -C₆ alkylaminocarbonyl substituted with 0-3R¹¹, benzoyl substituted with 0-3 R¹², phenoxycarbonyl substituted with 0-3R¹², phenylaminocarbonyl substituted with 0-3 R¹², or heteroarylcarbonyl. Examples of groups that, when administered to a mammalian subject, are cleaved to form a free hydroxyl, amino or sulfhydryl, may include hydroxy, amine or sulfhydryl protecting groups, respectively.

As used herein, the term "amine protecting group" means any group known in the art of organic synthesis for the protection of amine groups. Such amine protecting groups include those listed in Greene and Wuts, "Protective Groups in Organic Synthesis" John Wiley & Sons, New York (1991) and "The Peptides: Analysis, Synthesis, Biology, Vol. 3, Academic Press, New York (1981), the disclosure of which is hereby incorporated by reference. Any amine protecting group known in the art can be used. Examples of amine protecting groups include, but are not limited to, the following: 1) acyl types such as formyl, trifluoroacetyl, phthalyl, and p-toluenesulfonyl; 2) aromatic carbamate types such as benzyloxycarbonyl (Cbz) and substituted benzyloxycarbonyls, 1-(p-biphenyl)-1-methylethoxycarbonyl, and 9-fluorenylmethoxycarbonyl (Fmoc); 3) aliphatic carbamate types such as tert-butyloxycarbonyl (Boc), ethoxycarbonyl, diisopropylmethoxycarbonyl, and allyloxycarbonyl; 4) cyclic alkyl carbamate types such as cyclopentyloxycarbonyl and adamantyloxycarbonyl; 5) alkyl types such as triphenylmethyl and benzyl; 6) trialkylsilane such as trimethylsilane; and 7) thiol containing types such as phenylthiocarbonyl and dithiasuccinoyl.

The term "amino acid" as used herein means an organic compound containing both a basic amino group and an acidic carboxyl group. Included within this term are natural amino acids, modified and unusual amino acids, as well as amino acids which are known to occur biologically in free or combined form but usually do not occur in proteins. Included within this term are modified and unusual amino acids,such as those disclosed in, for example, Roberts and Vellaccio (1983) The Peptides, 5: 342-429, the teaching of which is hereby incorporated by reference. Modified or unusual amino acids which can be used to practice the invention include, but are not limited to, D-amino acids, hydroxylysine, 4-hydroxyproline, an N-Cbz-protected amino acid, ornithine, 2,4-diaminobutyric acid, homoarginine, norleucine, N-methylaminobutyric acid, naphthylalanine, phenylglycine, β-phenylproline, tert-leucine, 4-aminocyclohexylalanine, N-methylnorleucine, 3,4-dehydroproline, N,N-dimethylaminoglycine, N-methylaminoglycine, 4-aminopiperidine-4-carboxylic acid, 6-aminocaproic acid, trans-4-(aminomethyl)-cyclohexanecarboxylic acid, 2-, 3-, and 4-(aminomethyl)-benzoic acid, 1-aminocyclopentanecarboxylic acid, 1-aminocyclopropanecarboxylic acid, and 2-benzyl-5-aminopentanoic acid.

The term "peptide" as used herein means a compound that consists of two or more amino acids (as defined herein) that are linked by means of a peptide bond. The term "peptide" also includes compounds containing both peptide and non-peptide components, such as pseudopeptide or peptide mimetic residues or other non-amino acid components. Such a compound containing both peptide and non-peptide components may also be referred to as a "peptide analog".

The term "peptide bond" means a covalent amide linkage formed by loss of a molecule of water between the carboxyl group of one amino acid and the amino group of a second amino acid.

As used herein, "pharmaceutically acceptable salts" refer to derivatives of the disclosed compounds wherein the parent compound of formula (I) is modified by making acid or base salts of the compound of formula (I). Examples of pharmaceutically acceptable salts include, but are not limited to, mineral or organic acid salts of basic residues such as amines; alkali or organic salts of acidic residues such as carboxylic acids; and the like.

"Prodrugs" are considered to be any covalently bonded carriers which release the active parent drug according to formula (I) in vivo when such prodrug is administered to a mammalian subject. Prodrugs of the compounds of formula (I) are prepared by modifying functional groups present in the compounds in such a way that the modifications are cleaved, either in routine manipulation or in vivo, to the parent compounds. Prodrugs include compounds of formula (I) wherein hydroxy, amine, or sulfhydryl groups are bonded to any group that, when administered to a mammalian subject, cleaves to form a free hydroxyl, amino, or sulfhydryl group, respectively. Examples of prodrugs include, but are not limited to, acetate, formate, or benzoate derivatives of alcohol and amine functional groups in the compounds of formula (I); phosphate esters, dimethylglycine esters, aminoalkylbenzyl esters, aminoalkyl esters and carboxyalkyl esters of alcohol and phenol functional groups in the compounds of formula (I); and the like.

The pharmaceutically acceptable salts of the compounds of formula (I) include the conventional nontoxic salts or the quaternary ammonium salts of the compounds of formula (I) formed, for example, from nontoxic inorganic or organic acids. For example, such conventional non-toxic salts include those derived from inorganic acids such as hydrochloric, hydrobromic, sulfuric, sulfamic, phosphoric, nitric and the like; and the salts prepared from organic acids such as acetic, propionic, succinic, glycolic, stearic, lactic, malic, tartaric, citric, ascorbic, pamoic, maleic, hydroxymaleic, phenylacetic, glutamic, benzoic, salicylic, sulfanilic, 2-acetoxybenzoic, fumaric, toluenesulfonic, methanesulfonic, ethane disulfonic, oxalic, isethionic, and the like.

The pharmaceutically acceptable salts of the present invention can be synthesized from the compounds of formula (I) which contain a basic or acidic moiety by conventional chemical methods. Generally, such salts can be prepared by reacting the free acid or base forms of these compounds with a stoichiometric amount of the appropriate base or acid in water or in an organic solvent, or in a mixture of the two; generally, nonaqueous media like ether, ethyl acetate, ethanol, isopropanol, or acetonitrile are preferred. Lists of suitable salts are found in Remington's Pharmaceutical Sciences, 17th ed., Mack Publishing Company, Easton, Pa., 1985, p. 1418, the disclosure of which is hereby incorporated by reference.

The disclosures of all of the references cited herein are hereby incorporated herein by reference in their entirety.

Synthesis

The compounds of formula (I) can be prepared using the reactions and techniques described below. The reactions are performed in a solvent appropriate to the reagents and materials employed and suitable for the transformations being affected. It will be understood by those skilled in the art of organic synthesis that the functionality present on the molecule should be consistent with the chemical transformations proposed and this will sometimes require judgment as to the order of synthetic steps or selection of particular process scheme used from that shown below in order to obtain a desired compound of the invention. ##STR32##

Amine hydrochloride 1 is readily available via the procedure of Kettner and Shenvi (EP 0293881 A2).

There are numerous synthetic methods by which to prepare amide 2, however, competing with amide formation is the cyclization of 1 to afford a complex mixture containing the desired amide and the corresponding N-acylboroproline. Since purification at this stage is unfeasible, choosing the correct method for amide formation is crucial to obtaining 2 in a purity suitable for subsequent synthetic transformations.

Three methods are preferred for the preparation of 2. In the first, a solution of 1 in tetrahydrofuran or dichloromethane at 0° C. is treated sequentially with the desired acid chloride followed by two equivalents of triethylamine. The mixture is then allowed to warm to room temperature overnight. The second method is the mixed anhydride procedure of Anderson, et. al. (J. Am. Chem. Soc. 1967, 89, 5012). In this method the isobutyl mixed anhydride is generated by dissolving the carboxylic acid component in tetrahydrofuran and adding one equivalent of N-methylmorpholine. The solution is cooled to 0° C. and one equivalent of isobutyl chloroformate is added. After 5 minutes, a solution of 1 in chloroform is added, followed by the addition of one equivalent of triethylamine. The mixture is typically stirred at 0° C. for one hour followed by one to several hours at room temperature. The third method for amide formation is the hydroxybenzotriazole/DCC method of Konig and Geiger (Chem. Bet. 1970, 103, 788-98). Thus, to a solution of i and the carboxylic acid component in dimethylformamide or tetrahydrofuran at 0° C. is added N-methylmorpholine, 1-hydroxybenzotriazole hydrate (2 eq) and DCC (1.05 eq). The solution is allowed to warm to room temperature overnight.

The preferred method for the preparation of azide 3 is by reaction of 2 with sodium azide (1.1 eq) in dimethylformamide at 70° C. for 2 hours.

The azide displacement may also be performed prior to amide formation. This is the preferred method in cases where the rate of amide formation is slow relative to the rate of cyclization. Azide 4 is prepared by a modification of the procedure of Kettner and Shenvi (EP 0293881 A2) as shown in Scheme 2. Thus, bromide 5 is reacted with sodium azide, followed by homologation to give 6, chloride displacement to afford 7 and acidic hydrolysis to give 4. Amide formation between 4 and the carboxylic acid component then affords 3 directly. ##STR33##

Reduction of azide 3 to amine 8 may be accomplished by hydrogenation over precious metal catalysts. The preferred catalyst for this transformation is Pearlman's catalyst (palladium hydroxide on carbon). The amine is typically isolated as the hydrochloride salt. Isolation of 8 as the free base typically results in lowered yields. Salts of 8 which may confer superior physical properties may be preferred over the hydrochloride salt.

Formamidination of amine 8 may be accomplished using cyanamide. Due to the low reactivity of amine 8, however, the preferred method for this transformation is reaction with 4-dimethylamin-opyridine (DMAP) and aminoiminomethanesulfonic acid (AMSA, prepared by the method of Kim, et. al., Tetrahedron Lett. 1988, 29, 3183-6). This affords guanidine 9, which is isolated as the bisulfite or hydrochloride salt.

Cleavage of pinanediol ester 9 may be accomplished using anhydrous boron trichloride according to the procedure of Matteson and Ray (J. Am. Chem. Soc. 1980, 102, 7588). This method, however, is strongly Lewis acidic and leads to partial destruction of the substrate. The preferred method for water soluble boronic acids is a transesterification reaction that is run in the presence of excess phenylboronic acid. The free boronic acid 10 may then be isolated using cation exchange chromatography.

The isothiouronium functionalized analogs 11/12 are prepared from bromide 2 according to the procedure of Kettner and Shenvi (EP 0293881 A2).

Inhibitors containing a sulfonamide in place of a carboxamide are prepared from either 1 or 4 by reaction with a sulfonyl chloride in the presence of a hindered amine (Scheme 3). The product sulfonamide 13 is then converted to the guanidinium 14 or isothiouronium 15 in the same manner as the corresponding carboxamides. ##STR34##

Inhibitors containing the borolysine moiety are prepared analogously to those containing boroarginine according to Kettner and Shenvi (EP 0293881 A2).

Novel biaryls synthesized in this invention are prepared through palladium catalyzed coupling of an appropriate arylmetal species to the aryl halide of choice using the methods described in Negishi, et. al., Org. Synth. 1987, 66, 67-74, and references cited within.

Synthetic approaches toward construction of pyrroles are numerous: R. J. Sundberg in "Comprehensive Heterocyclic Chemistry", A. R. Katritzky (Ed.), Pergamon Press, New York (1984), Vol. 4, p. 705; Synthesis, 1946, 281. The following discussion is restricted to the most common and reliable methods towards the synthesis of pyrroles within the general scope of the invention.

Compounds where R¹ is a pyrrole can be synthesized as shown on Scheme 4. ##STR35##

Starting material diketone 16 may or may not have its substituents R¹³⁻¹⁶ in final form as defined in the scope. These substituents might be in protected forms or in the form of suitable precursors which make the heterocyclic portion, for example, amenable to synthesis. These precursor forms can then be converted to their final forms later on in the synthesis using procedures familiar to one skilled in the art.

The cyclization condensation of 1,4-dicarbonyl compounds with ammonia, primary amines or related compounds, the Paal-Knorr reaction, is one of the most general and widely applicable pyrrole syntheses, R. A. Jones and G. P. Bean, "The Chemistry of Pyrroles", Academic Press, London, 1977; p. 77-81. The generality of this approach is primarily determined by the availability of the dicarbonyl precursors, 16, as illustrated by Scheme 4. By heating such diketones with ammonia or amines in a solvent like benzene, toluene or methylene chloride with a catalyst such as sulfuric acid, acetic acid, p-toluenesulfonic acid, alumina or even titanium tetrachloride, pyrroles like 17 may be prepared.

Subsequent alkylation of pyrrole 17 with a bromoester, for example, leads to the alkylated heterocycle 18. Alkylation conditions include either first deprotonating with NaH or KH in DMF followed by addition of the alkylating agent or simply stirring the heterocycle with the alkylating agent in an inert solvent such as DMF or DMSO at 0° C. to 100° C. in the presence of an acid scavenger such as K₂ CO₃.

Saponification of ester 18 followed by coupling aminoboronic ester 1 or 19 as discussed previously yields compound 20. This bromide may be either elaborated to the lysine side-chain 21 (X=1) or if X=O, into the corresponding ornithine side-chain or any other side-chain discussed previously. Subsequent hydrolysis of the boronic ester yields the boronic acid as discussed previously too.

The cyclization of diynes 23 with amines has been reported and an adaptation of this method is shown in Scheme 5 (K. E. Schulte et al., Chem. Ber (1965) 98; A. J. Chalk Tet. Lett. (1972) 3487). The diynes are made via transition metal catalyzed coupling of alkynes, i.e., the Cadio-Chodkiewicz reaction (W. Chodkiewicz Ann. Chim, (Paris) (1957) 2 81 g). ##STR36##

Furans (27) have been converted directly to pyrroles by treatment with amines but the harsh conditions required (400° C./Al₂ O₃) precludes its generality. 2,5-Dialkoxytetrahydrofurans (29) have been more commonly employed as furan (or 1,4-dicarbonyl) equivalents and react readily with aliphatic or aromatic amines (and even weakly nucleophilic sulfonamides) to give pyrroles as shown in Scheme 6 , J. W. F. Wasley and K. Chan, Synth. Commun. 3, 303 (1973). Although commercially available 2,5-dialkoxytetrahydrofurans (29) (R¹ ═R² ═H))generally restrict one to preparing 1-substituted pyrroles, more highly substituted systems may be obtained by a three-step alcoholysis of the appropriate furans (27) to the more highly substituted 2,5-dialkoxytetrahydrofurans (29) as shown in Scheme 6, N. L. Weinberg and H. R. Weinberg, Chem. Rev., 68, 449 (1968); N. Elming, Adv. Org. Chem., 2, 67 (1960).

The Hantzsch synthesis utilizes the condensation of β-haloketones (30a) and β-ketoesters (31) in the presence of ammonia or a primary amine to give pyrroles such as (32), as shown in Scheme 7, A. Hantzsch, Chem. Ber., 23, 1474 (1980); D. C. von Beelen, J. Walters, and S. von der Gen, Rec Tray. Chem. 98, 437 (1979). Among the numerous modifications reported over the years, the substitution of (30a) with the readily available α-hydroxyaldehydes or nitroalkenes has expanded the versatility and generality of this important method, D. M. McKinnon, Can. J. Chem. 43, 2628 (1965); H. George and H. J. Roth, Arch. Pharm. 307, 699 (1974); C. A. Grok and K. Camenisch, Helv. Chem. Acta, 36, 49 (1953). ##STR37##

The closely related Knorr condensation involves the reaction between amino carbonyl compounds (or their precursors) and carbonyl (or dicarbonyl) compounds, J. M. Patterson, Synthesis, 282 (1976). Representative methods for preparing substituted pyrroles (35 and 38) are shown by Scheme 8, equations a) and b), S. Umio et al., Jap. Pat. 7018653, Fujisawa Pharmaceutical Co., Ltd., 1970 (C. A. 73, 77039, 1970); K. Tanaka, K. Kariyone, S. Umio, Chem . Pharm. Bull. (Tokyo)), 17, 611 (1969).

The elaboration of an appropriately functionalized pyrrole is another method for preparing pyrroles of general formula I. Methyl (or ethyl) 5-formyl-1H-pyrrole-2-carboxylate (43) is a particularly useful intermediate with regards to pyrroles claimed in this invention and has been prepared by a number of methods as shown by Scheme 9, eq. a, W. A. Davies, A. R. Pinder and I. G. Morris, Tetrahedron 18, 405 (1962); Org Syn., vol 36, p. 74; Org. Syn., vol. 51.

More recently, Ullrich has extended the Vilsmeyer-Haack formylation of pyrroles to include vinylogous systems such as (46) by using the 3-(N,N-dimethylformamide derivative, as shown by Scheme 9, eq. b, F. W. Ullrich and E. Breitmaier, Synthesis, 641 (1983); W. Heinz, et al., Tetrahedron, 42, 3753 (1986).

An especially attractive approach to pyrroles claimed in this invention has recently been reported, whereby lithiation of the 6-dimethylamino-1-azafulvene dimer (49) followed by treatment with an appropriate electrophile and subsequent hydrolysis leads to 5-substituted pyrrole-2-carboxaldehydes (51), as illustrated in Scheme 10, J. M. Muchowski and P. Hess, Tetrahedron Lett., 29, 777 (1988). The carboxylic acid, ester and aldehyde side-chains depicted in Schemes 9-10 can be readily converted to R¹³⁻¹⁶ by methods familiar to one skilled in the art. ##STR38##

A general and versatile approach to pyrazoles (R¹ ═pyrazole) involves condensation of a 1,3-difunctional compound (usually dicarbonyl) with hydrazine or its derivatives, as shown in Scheme 11 for pyrazoles of the formula 53 and reviewed by G. Corspeau and J. Elguerv, Bull. Soc. Chim. Fr., 2717 (1970). Rarely have pyrazoles have been prepared in which the N-N bond is the last step of the ring closure, J. Elguerv in Comprehensive Heterocyclic Chemistry, S. R. Katritzky (Ed.) Pergamon Press, New York, Vol. 5 (1984), p. 274; J. Barluenga, J. Chem. Soc, Perkin Trans.1, 2275 (1983). ##STR39##

The condensation of 1,3-dicarbonyl compounds with hydrazine hydrate derivatives is generally carried out by admixture of the two components in a suitable solvent like a lower alcohol, ether, or THF at 0° C. to the reflux temperature for 1-18 hours.

The synthesis of 1,3-dicarbonyl compounds has received considerable attention in the literature and most of the major approaches towards 1,3-diketones 52 of interest in this invention are illustrated by Scheme 12. ##STR40##

Esters 54a can be reacted with ketones 54 using bases like sodium ethoxide, sodium hydride or sodium amide in a suitable solvent like alcohol, DMF, DMSO or benzene at 0° C. to reflux for 4-18 hours with 30-70% efficiency, J. M. Sprague, L. J. Beckham and H. Adkins, J. Amer. Chem. Soc., 56, 2665 (1934). Metallation of hydrazines 55 with n-BuLi followed by reaction with carboxylic acid chlorides and subsequent hydrolysis affords 52, D. Enders and P. Wenster, Tetrahedron Lett., 2853 (1978). Metallation of 54 with the non-nucleophilic mesityl lithium followed by acylation also affords 52, A. K. Beck, M. S. Hoelstein and D. Seebach, Tetrahedron Lett., 1187 (1977); D. Seebach, Tetrahedron Lett., 4839; (1976).

As shown in Scheme 12, equation b, the addition of Grignard reagents to β-keto carboxylic acid chlorides may be limited to monoaddition at low temperatures to provide 52, C. D. Hurd and G. D. Kelso, J. Amer. Amer. Soc. 62, 1548 (1940); F. Sato, M. Trone, K. Oyuro, and M. Sato, Tetrahedron Lett. 4303 (1979). Lithium dialkyl copper reagents (R² CuLi) have also been used, Luong-Thi and Riviero, J. Organomet. Chem. 77, C52 (1974). Analogously, addition of alkyllithium reagents (R¹⁵ Li) to the monoanions of β-keto esters 57 also give rise to 1,3-diketones, S. N. Huckin and L. Weiler, Can. J. Chem, 52, 1379 (1974).

Eschenmoser has demonstrated a synthesis of β-diketones through a sulfur extrusion reaction of keto thioesters 58 with tributylphosphine, triethylamine and lithium perchlorate, S. Eshenmoser, Helv. Chim. Acta, 54, 710 (1971).

The rearrangement of α,β-epoxy ketones 59 to β-diketones 52 catalyzed by Pd° has been reported, R. Noyori, J. Amer. Chem. Soc. 102, 2095 (1980).

Mixed anhydrides such as 61, available from carboxylic acids 60 and trifluoroacetic anhydride, have been shown to acrylate alkynes 62 to produce the enol trifluoroacetate of a β-diketone 63. Transesterification by refluxing with methanol liberates the β-diketone 52, A. L. Henne and J. M. Tedder, J. Chem. Soc. 3628 (1953). ##STR41##

Compounds where R¹ =imidazole, such as 65, are readily available by any of a number of standard methods. For example, acylaminoketone 64 can be cyclized with ammonia or equivalents thereof, D. Davidson, et al., J. Org. Chem., 2, 319 (1937) to the corresponding imidazole as shown in Scheme 13. The corresponding oxazole 66 can also be converted to imidazole 65 by action of ammonia or amines in general, H. Bredereck, et. al., Bet., 88, 1351 (1955); J. W. Cornforth and R. H. Cornforth, J. Chem. Soc., 96, (1947).

Several alternative routes to imidazoles 65 are illustrated in Scheme 14. As shown in Scheme 14 equation a), reaction of the appropriate R¹³ substituted imidate esters 67 with an appropriately substituted α-hydroxy- or α-haloketone or aldehyde 68 in ammonia leads to imidazoles of formula 65, P. Dziuron, and W. Schunack, Archive, Pharmaz., 307 and 470 (1974).

The starting imidazole compounds 65 wherein R¹³ is hydrogen can be prepared as shown in equation b) by reaction of the appropriate R¹³ -substituted imidate ester 67 with α-aminoacetaldehyde dimethyl acetal, M. R. Grimmett, Adv. Heterocyclic Chem., 12, 103 (1970).

As shown in equation c), imidazole 72 (wherein R¹³ =hydrogen and CH₂ OH) can be prepared by treatment of the imidate ester 67 with 1,3-dihydroxyacetone 71 in ammonia by the procedure described in Archive der Pharmazie, 307, 470 (1974). Halogenation of imidazole 72 or any imidazole wherein R¹³ is hydrogen is preferably accomplished by reaction with one to two equivalents of N-halosuccinimide in a polar solvent such as dioxane or 2-methoxyethanol at a temperature of 40°-100° C. for 1-10 hours.

Compounds of formula 73 can also be prepared from 70 by reaction with formaldehyde as described in E. F. Godefroi, et al., Recueil, 91, 1383 (1972) followed by halogenation as was described above.

As shown in equation d) the imidazoles 65 can also be prepared by reaction of R¹³ substituted amidines 74 with an α-hydroxy- or α-haloketone or aldehyde 68 as described by F. Kunckel, Ber., 34, 637, (1901).

As shown in equation e), preparation of the nitroimidazoles (65, R¹³ =NO₂) is preferably accomplished by heating the appropriate starting imidazole in a 3:1 mixture of conc. sulfuric acid/conc. nitric acid at 60°-100° C. for 1-6hours. Nitration of the imidazole can be achieved by first converting the hydroxmethylimidazole to the corresponding chloromethylimidazole 75 employing thionyl chloride or oxalyl chloride. Nitration, as described above, followed by hydrolysis provides the nitroimidazoles 77.

Imidazoles 80 where R¹³ =CN can be prepared as shown in equation f) by reaction of R¹³ substituted ortho esters, ortho acids or aldehydes (followed by oxidation of the aldehyde) with diaminomaleonitrile 79 by the procedure described by R. W. Begland et al., J. Org, Chem., 39, 2341 (1974). Likewise, R¹³ substituted imidate esters 67 also react with diaminomaleonitrile to give 4,5-dicyanoimidazoles 80. The nitrile groups can be further elaborated into other functional groups by methods familiar to one skilled in the art.

Compounds wherein R¹³ =alkyl of 1-6(straight or branched), phenyl, phenalkyl where alkyl is 1-3 carbon atoms, etc. and another R¹³ =CH₂ OH can be prepared as shown in equation g). The imidazoles 83 were prepared as described in L A. Reiter, J, Org. Chem., 52, 2714 (1987), Hydroxymethylation of 83 as described by U. Kempe, et al. in U.S. Pat. No. 4,278,801 provides the hydroxymethylimidazoles 84.

The CH₂ OH group, as in imidazolemethanol 72, is a versatile synthon for other functional groups. Scheme 15 shows some of these transformations, all of which are familiar to one skilled in the art. ##STR42##

A suitably protected imidazole 85 may undergo selective halogen-metal exchange followed by quenching with electrophiles to yield trisubstituted imidazoles (Scheme 16) (M. Groziak and L. Wei J. Org. Chem. (1992) 57, 3776). This strategy can be used to add several R¹³ groups onto the imidazole ring. By changing the order in which the electrophiles are added, one may change the position to which the electrophile gets attached onto the imidazole ring. ##STR43## where (R¹³)⁺ is a suitable electrophilic precursors to R¹³.

The pyrazoles and imidazoles disclosed previously and other heterocycles which will be mentioned later in this specification may undergo alkylation onto a nitrogen ##STR44## atom just as the pyrrole in Scheme 4 by simply stirring a mixture of the heterocycle 88 and alkylbromide, iodide, mesylate or tosylate 89 in the presence of an acid scavanger such as potassium carbonate in an inert solvent such as THF or DMF for several hours to several days at room temperature or up to the reflux temperature of the solvent (Scheme 17).

Another way to make 90 involves first deprotonation of the N--H of heterocycle 88 with a base such as NaH, KH, n-BuLi, t-BuLi, etc., followed by displacement of the X-leaving group of 89 to yield 90.

This sequence can be performed in inert solvents such as ether or THF. NaH and KH can also be employed in DMF and DMSO at room temperature or at a higher temperature. Alkylation sometimes yields regioisomers when more than one nitrogen atom is present in the heterocycle. These isomers can be separated by standard methods such as crystallization or chromatography. Once alkylated, the Y group can be coupled to the boronic acid moiety and all protecting groups removed to yield compounds of Formula I by procedures described previously.

Compounds where R¹ =1,2,4-triazole can be prepared by the route of H. Paul, G. Hilgetag and G. Jahnchen, Chem. Ber., 101, 2033 (1968) which is depicted in Scheme 18. Imidate ester 92 is formed from nitrile 91 by the method of P. Keynaud and R. D. Moreau Bull. Soc. Chim. France, 2997 (1964). Hydrazide 99 is easily ##STR45## prepared via the action of hydrazine on the corresponding methyl ester precursor. It is understood that R¹³ of 91 and 94 do not necessarily have to be in their final form, for example. In each case, they can exist as either a protected species or in the form of a precursor to R¹³.

Alkylation of triazole 96 yields two isomeric products 97 and 98 when the R¹³ groups are not identical. These intermediates can be converted into final products in the usual fashion as shown in Scheme 19. ##STR46##

The regioselective syntheses of both 97 and 98 are shown in Scheme 20. Imidate ester 93 is reacted with hydrazine to form amidrazone 103. Alkylation with methyl μ-bromoacetate yields 104. Ring closure with either an ortho-ester, acid chloride or anhydride yields triazole 98. For a similar triazole synthesis, see David B. Reitz, European Patent Application 508, 445, published 14.10.92., G. D. Searle & Co. For schemes 20, 21 and 22, the different R¹³ groups are differentiated from one another by the placement of a prime symbol next to one of the R¹³ groups, i.e. R^(13'). ##STR47##

Yet another regioselective synthesis of 97 or 98 is depicted in Scheme 21 following a similar sequence as was shown in Scheme 20 (D. B. Reitz, ibid.). ##STR48##

1,2,4-Triazoles also undergo selective metalation at the 5-position when the nitrogen at the 1-position is suitably protected. The metallated triazole can then be quenched through the addition of an electrophile to result in a newly functionalized triazole at the 5-position. Suitable protecting groups are benzyl and trityl. (D. K. Anderson, et al., J. Heterocyclic Chem., 23, 1257 (1986) as well as diethoxymethyl (S. Ohta, et al., Chem. Pharm. Bull., 41, 1226 (1993). The 3-position can also be metallated if the 5-position is suitably protected (S. Ohta et al., ibid.). Thus here we have two other methods for introducing R¹³ substituents at the 5- or 3-positions of the 1,2,4-triazoles.

Compounds where R¹ =1,2,3-triazole can be synthesized via the 1,3-dipolar cycloaddition of an azide to an alkyne as shown in Scheme 22 (for an example of this cycloaddition reaction, see W. Kirmse and L. Horner Justus Liebigs Ann. Chem. (1958) 614, 1). ##STR49##

Compounds where R¹ =tetrazole can be synthesized by the methods outlined in Scheme 23. In line a, three methods are given for the conversion of a nitrile into a tetrazole (ammonium chloride/sodium azide: W. G. Finnegan et al., J. Am. Chem. Soc. 1958, 80, 3908; trialkyltin azides: J. G. Luitjen et al., Rec. Tray. Chim. Pays-Bas; dialkyltin oxide: S. Wittenberger and B. G. Donner, J. Org. Chem., 1993, 58, 4139).

In Scheme 23, line b, two procedures are given for the regioselective synthesis of 1,5-disubstituted tetrazoles (DEAD, Ph₃ P, TMSN₃ : J. V. Duncia, M. E. Pierce, J. B. Santella III, J. Org. Chem. 1991, 56 2395; Tf₂ O/NaN₃ : E. W. Thomas Synthesis, 1993, 767) which can be more difficult to synthesize due to the steric crowding of the substituents.

Compounds where R¹ is an oxazole may be synthesized by a variety of methods including those outlined in Scheme 24. The oldest synthesis and one of the most versatile is shown on line a), namely the cyclodehydration of 2-acylaminoketones (The Robinson-Gabriel Synthesis) (see I. J. Turchi in Oxazoles, Turchi, I. J., ed. John Wiley and Sons, New York (1986) p. 1). The 2-acylaminoketone starting materials may be synthesized from the Dakin-West reaction and modifications thereof (G. H. Cleland and F. S. Bennett Synthesis (1985) 681 and references therein). Some cyclodehydration agents include PCl₅, H₂ SO₄, P₂ O₅, SOCl₂, etc). ##STR50##

R^(a), R^(b) and R^(c) are equal to R¹³ which is described in the scope of this application. R¹³ in Scheme 24 does not have to be in finalized form as it appears in the scope, but can be in protected form or in the form of suitable precursors. It is understood that only when the entire molecule of formula I is synthesized do all of the substituents have to appear in their final forms as stated in the scope. Protected forms and suitable precursors to R¹³ are readily recognized by one skilled in the art of organic synthesis.

In line b, the reaction of α-acylketones 131 with ammonium acetate/acetic acid also yields oxazole 130 (D. Davidson, M. Weiss, M. Jelling J. Org. Chem. (1937), 2 328). In line c, we find the regioselective formation of oxazole 130 from the reaction of an α-haloketone 134 with amide 133 (R. Lakham, B. Ternai, Adv. Heterocycl. Chem. (1974) 17, 99; I. J. Turchi, M. J. S. Dewar, Chem. Rev. (1975), 75, 389). Acid chlorides 135 react with oximes 136 to yield after a [3,3] sigmatropic rearrangement (138) oxazole 130 as shown in line d (G. S. Reddy and M. V. Bhatt Ind. J. Chem. (1981) 208, 322; M. V. Bhatt, G. S. Reddy Tet. Lett. (1980) 21, 2359). In line e, μ-azidoketones (140), after reaction with triphenylphosphine to yield 141, react with acid chloride 135 to yield oxazole 130 (E. Zbiral, E. Bauer, J. Stroh Monatsh. Chem. (1971) 102, 168). Finally, oxazoles undergo deprotonation with strong bases such as n-BuLi at the 2-position when the 4 and 5 positions are blocked and after quenching with an electrophile can yield oxazole 130 (R. Schroder, V. Schollkopf, E. Blume, I. Hoppe Liebigs Ann. Chem., (1975) 533). As stated earlier, R¹³ can be either in final form as defined in the scope of this application or in the form of precursor functionality which later on can be elaborated into final form by methods familiar to one skilled in the art. This holds true not only for the oxazoles discussed here, but for all of the other heterocyclic systems in this application where R¹³ appears as substituents.

Oxazoles are most readily brominated at the 5-position followed by the 4-position and finally the 2-position. A brominated oxazole (as well as other brominated heterocycles in this application) can undergo aryl cross-coupling reactions catalyzed by transition metals to yield aryl-or heteroaryl-substituted oxazoles (See for example E.-I. Negishi; A. O. King; N. Okukado J. Org. Chem. (1977) 42, 1821).

Compounds where R¹ is an isoxazole may be synthesized by the methods outlined in Scheme 25. In line a, reaction of 1,3-diketone 143 with hydroxylamine yields oxazoles 144 and 145. Nitrile oxide 146 can also add across the triple bond of alkyne 147 to yield isoxazoles 144 and 145. (See P. Grunanger and P. Vita-Finsi Isoxazoles, v. 49 pt. 1 of The Chemistry of Heterocyclic Compounds, E. C. Taylor and A. Weissberger, eds., John Wiley and Sons (New York: 1991) p. 126). ##STR51##

As discussed previously R^(a), R^(b) and R^(c) in Scheme 25 are again equal to R¹³ and are not necessarily in final form as they appear in the scope of this application.

Compounds wherein R¹ is a thiazole may be synthesized by the method depicted in Scheme 26, which mimics the route of Scheme 24c) describing a route for oxazoles. Thus thioamide 148 reacts with α-halocarbonyl compound 134 to yield thiazole 149. Again as for the oxazole, R^(a), R^(b), and R^(c) have the same definitions. For the synthesis of thiazoles, by the route depicted in Scheme 26, see G. Vernin "General Synthetic Methods for Thiazole and Thiazolium Salts" in Thiazole and Its Derivatives, J. V. Metzger, ed., volume 34. pt. 1 in The Chemistry of Heterocyclic Compounds, A. Weissberger and E. C. Taylor, eds. John Wiley and Sons (New York:1979) p. 180. ##STR52##

Compounds wherein R¹ is a 1,2,5-thiadiazole may be synthesized by the methods shown in Scheme 27. Diamine 150 may be reacted with sulfur monochloride to yield 1,2,5-thiadiazole 151. Likewise, α-diketone 152 may be converted into bisoxime 153 which also reacts with S₂ Cl₂ to yield 151 (L. M. Weinstock, P. Davis, B. Handelsman, R. Tull J. Org. Chem. (1967) 32, 2823). Z is defined in Scheme 24. ##STR53##

Compounds wherein R¹ is a 1,2,4-thiadiazole may be synthesized by the method depicted in Scheme 28. Oxidation of thioamide 154 with hydrogen peroxide yields S-oxide 155 which must be stored at 0° C. Further reaction of the S-oxide intermediate with thioamide 156 yields thioacylamidine 157 which cyclizes to product 158 (V. Goerdeler, H. Porrmann Chem. Ber. (1962) 95, 627). R^(a) and R^(b) are as defined previously in Scheme 24.

Compounds where R¹ is a furan may be synthesized by the methods shown in Scheme 29, but as understood by one skilled in the art, not limited thereto, as in the case as for all of the schemes in this patent application. In line a, cyclodehydration of 1,4- dicarbonyl compound 159 yields furan 160 (L. D. Krasnoslobodskaya, Ya. L Gol'dfarb Russ. Chem. Rev. (Engl. Trans.) 1969, 38, 389). In line b, α-bromoketone or aldehyde 161 protected as its dimethyl ketal or acetal reacts with trimethylsilylenol ether 162 to yield intermediate 163 which cyclizes to furan 160 (T. Mukaiyama, H. Ishihara, K. Inomata Chem, Lett., 1975, 527). R^(a), R^(b), R^(c), and R^(d) are R¹³ which is described in the scope of this application and with similar limitations as were described under Scheme 24 for R¹³ with regards to being in final form or not.

Compounds where R¹ is a thiophene may be synthesized by the methods shown in Scheme 30. In line a, 1,4-dicarbonyl compound 159 is reacted with a phosphorous sulfide (phosphorous pentasullfide, phosphorous trisulfide, phosphorous heptasulfide, etc.) to yield thiophene 164 (H. D. Hartough, Chem. Heterocycl. Compd., 1952, 3, 1). The dicarbonyl compound 159 also reacts with H₂ S to favor thiophenes at lower temperatures (-50° C.) (F. Duus Tetrahedron, 1976, 32, 2817). Reaction of alkenes 165 or 166 (line b) with sulfur and heat also yield thiophene 164 (A. S. Broun, M. G. Voronkov J. Gen, Chem. USSR, (Engl. Trans.) (1947) 17, 1162; M. g. Voronkov, A. S. Broun, ibid, (1948) 18, 700; J. Schmitt, M. Suquet, R. Fallard (C. R. Hebd. Seances Acad, Sci. (1956) 242, 1738. R^(a), R^(b), R^(c) and R^(d) are as defined in Scheme 29. ##STR54##

Compounds where R¹ is a pyridine may be synthesized by the methods shown in Scheme 31. It is to be understood that each scheme and each reaction has its own scope and limitations and that no one synthesis is universally applicable. It is also to be understood that one skilled in the art will be able to determine which synthesis is best suited for his or her needs. In line a, reaction of enamine 167 with ethynyl ketone 168 will cyclize to pyridine 170 (F. Bohlmann, D. Rahtz Chem. Ber. (1957) 90,, 2265). Enamino ketones 171 (line b) condense with 1,3-diketones or beta-keto esters 172 to yield pyridine 174 where R is alkyl, aryl or alkoxy and aryloxy (N. K. Kachetkov, A. Gonsales, A. Nesmeyanov Dokl. Akad, Navk, SSSR (1951) 79, 609; S. Auricchio, R. Bernardi, A. Ricca Tet. Lett. (1976) 9831; H. Henecka Chem. Ber. (1949) 82, 41).

The Hantsch dihydropyridine synthesis can be used in the synthesis of pyridines as shown in line c. There are many modifications of this synthesis of which only one is shown. Reaction of 175 with beta-aminocrotonate 176 yields dihydropyridine 177 (F. Bassett, H. Meyer, E. Wehinger Angew. Chem. Int. Ed. Engl. (1981) 20, 762). Further oxidation with, for example, dilute nitric acid yields pyridine 178 where R and R¹ can be different alkoxy groups (E. Knoevenagel, W. Rushhaupt Ber. (1898) 31 1025). Cycloaddition of oxazole 179 with alkene 180 can also yield a pyridine (182) (M. Ya Karpeiskii, V. L. Florent'ev Russ. Chem. Rev. (Engl. Trans.) (1969) 38, 540; R. Lakhan, B. Ternai Adv. Heterocyl. Chem. (1974) 17, 99). In all of these pyridine synthesis, R^(a), R^(b), R^(c), and R^(d) are as described for Scheme 29. All of the substituents around the pyridine ring can be in final form or in the form of a precursor to a given functional group as would be recognized by one skilled in the art. Finally, in line e, hydroxypyridines, such as 183, may be triflated and coupled with an aryl-or heteroarylboronic acid or aryl-or heteroaryltrialkylstannane using a transition metal catalyst such as Pd to yield aryl or heteroarylpyridinecarboxylic acids, such as 186. This in turn may be coupled to aminoboronic acid esters as discussed previously to yield compounds of Formula I. Halogens, such as Br or I may be used instead of triflate in compound 184 to undergo what is known as the Suzuki coupling reaction. R and R^(1') in line e) are any of the allowed phenyl substituents in the scope of this application (Suzuki reactions: A. Suzuki Pure Appl. Chem. (1985) 57, 1749). ##STR55##

Compounds where R¹ is a pyridazine may be synthesized by the routes shown in Scheme 32. Reaction of 1,4-carbonyl compound 187 with hydrazine yields pyridazine 188. If the 1,4-dicarbonyl compound is saturated as in line b (compound159), then the product from the reaction with hydrazine 189 must be oxidized to yield pyridazine 188 (K. C. Nicolaou, W. E. Barnette, R. L. Magolda J. Am. Chem. Soc. (1979) 101, 766; ##STR56## M. Tisler, B. Stanovnik "Pyridazines and their Benzo Derivatives" in A. R. Katrizky, C. W. Rees Comprehensive Heterocyclic Chemistry, v.3 (Pergamon Press: Oxford), 1984, p. 45). Halopyridazines or hydroxypyridazines may also undergo the same aromatic cross-coupling reactions as were described for pyridines. R^(a), R^(b), R^(c) and R^(d), etc., are defined the same as in the pyridine case.

Compounds wherein R¹ is a pyrimidine may be synthesized by the methods shown in Scheme 33. Reaction of 1,3-dicarbonyl compound 190 with amidine 191 yields pyrimidine 192 (D. J. Brown, S. F. Mason The Pyrimidines in A. Weissberger ed. The Chemistry of Heterocyclic Compounds, (John Wiley: New York) 1962, p. 31). ##STR57## Reaction of amidine 191 with 193 also yields pyrimidines (P. Schenone, L. Sansebastiano, L. Mosti J. Heterocyclic Chem. (1990) 27, 295). R^(a), R^(b), R^(c), and R^(d) are as defined previously in Scheme 32. Halopyrimidines or hydroxypyrimidines may also undergo the same aromatic cross-coupling reactions as were described for pyridines. ##STR58##

Compounds in which R¹ is a 1,2,4-triazine may be synthesized by the procedures outlined in Scheme 34. In line a, 1,3-dicarbonyl compound 194 is condensed with amidrazone 195 to yield triazine 196 (H. Neunhoeffer and P. F. Wiley Chemistry of 1,2,3-Triazines and 1,2,4-Triazines and Pentazines, v. 33 in A. Weissberger, E. C. Taylor, eds., The Chemistry of Heterocyclic Compounds John Wiley and Sons (New York: 1978) pp 194-200 and p. 524). In line b, cyclization of acylhydrazone 197 with ammonia or ammonium acetate leads to triazine 196 (H. Neunhoeffer, P. F. Wiley, ibid., p. 196, 197). In line c, reaction 1,2-dicarbonyl compound 194 with oxalamidrazonates 198 yields 1,2,4-triazine ester 199. Saponification of 199 yields 200 which can be decarboxylated to yield 1,2,4-triazine 201 (H. Neunhoeffer, P. F. Wiley, ibid., p. 526). R^(a), R^(b), and R^(c) are as defined in the pyridine case. Halotriazines or hydroxytriazines may undergo the same aromatic cross-coupling reactions as were described earlier for pyridines.

Compounds in which R¹ is as described in lines k and l in the scope of this application may be synthesized by the methods described in Scheme 35. If heterocycle --J--K--L--M--Q-- 202 contains a bromine, iodine or a hydroxyl group (which can be triflated) designated by X, then it can undergo a Suzuki coupling to yield 204 where u is 0 (A. Suzuki, ibid) (Scheme 35, line a). If instead of B(OH)₂ a trialkyltin group is present, then a Stille coupling can be performed when X=triflate (J. K. Stille Angew. Chem. Int. Ed. Engl. (1986) 25 508; J. K. Stille Pure Appl. Chem. (1985) 57, 1771). ##STR59## The X and B(OH)₂ (or trialkyltin) moieties may be reversed so that now X=B(OH)₂ (or R₃ Sn) and the phenyl of 203 contains halogen or triflate group. The same coupling procedures may be used in synthesizing compounds where R¹ is described by line 1 and u is 0 as were used in synthesizing compounds where R¹ is described by line k and u is 0.

When u is not 0, heterocycle 205 and its six-membered ring counterpart --C--W--R--T--U--V-- (described in line 1) must be synthesized from scratch by the methods described heretofore, with the --(CH₂)_(u) -Phenyl-(CH₂)_(m) CO₂ R group being one of the substituents in final or precursor form. If heterocycle 205 contains an N--H which is alkylatable, then alkylation with 206 where X is Cl, Br, I, mesylate tosylate or triflate yields 207 (Scheme 35, line b). The esters 204 and 207 can then be hydrolyzed to the free acid and coupled with aminoboronic acid ester derivative as described in Scheme 4, for example, to yield boronic acid esters which can also be hydrolyzed to the corresponding free boronic acid products.

A general method (Scheme 36) for the synthesis of 4-carboxydihydroheterocycles (oxazolines, thiazolines, imidazolines) utilizes the condensation of an α-amino acid ester (210) with an imidate (211) to provide 212, see: Meyers, A. I.; Hanagan, M. A.; Mazzu, A. L. Heterocycles 1981, 15, 361; Meyers, A. I.; Whitten, C. E. Heterocycles 1976, 1, 1687; North, M.; Pattenden, G. Tetrahedron 1990, 46, 8267; Jones, R. C. F.; Ward, G. J. Tetrahedron Lett. 1988, 29, 3853. In the case where R²⁰ =H, the cyclization might be conducted with trimethyl orthoformate instead of 211, see: Martin, P. K. et al. J. Org. Chem. 1968, 33, 3758. For compounds that are substituted only at the 2-position of the heterocycle, serine or cysteine might be used as the amino acid ester partner. The dihydroimidazole-based materials would be prepared from an N.sup.α -monoprotected diaminopropionic acid to prevent tautomerization of the double bond once the cyclic system of 212 has been formed, see: Martin, P. K. et al. J. Org. Chem. 1968, 33, 3758. Hydrolysis of the ester then affords carboxylic acid 213. ##STR60##

It may be desirable to prepare more highly substituted heterocycles as well (Scheme 37). An approach to the oxazoline class could utilize reaction between the anion of 215 and formaldehyde to provide adducts 216 as recorded by Kanemasa, S. et al. Tetrahedron Lett. 1993, 34, 677 and Ito, Y. et al. Tetrahedron 1988, 44, 5253. Hydrolysis of the imine should deliver 217, an example of an α-substituted α-amino acids, as a mixture of isomers. Condensation as before with imidate (211) should generate cyclic moieties of general structure 218 which are hydrolyzed to 219.

The corresponding thiazolines should be available by installing a sulfhydryl group prior to cyclocondensation. To that end, N-protection of 217, followed by reaction with a sulfur nucleophile, a thiol ester or an inorganic salt thereof, based on the work reported by Mitsunobu, O. Synthesis 1981, 1, and Yuan, W. et al. J. Med. Chem. 1993, 36, 211, should provide the substituted cysteine (220) upon premoval of the N-protecting group. Subsequent reaction with the imidate should deliver 221 and ultimately 222, after hydrolysis of the ester. ##STR61##

The imidazolines should be obtained via the condensation described by Jones, R. C. F.; Ward, G. J. Tetrahedron Lett. 1988, 29, 3853, of a suitable diamino acid with imidate 211. The preparation parallels the sequences discussed above where the anion of 215 would be expected to generate adduct 223 as described by Gilbert, I. et al. Tetrahedron Lett. 1991, 32, 2277. Manipulation of the protecting groups and implementation of the aforementioned cyclization should give imidazoline 225 which may be converted to the corresponding carboxylic acid 226.

Using an analogous synthetic sequence (Scheme 38), the polysubstituted versions of these heterocycles should also be accessible. For the oxazo- or imidazo- type compounds, reaction of the anion of 215 with an electrophile 227 should deliver 228, as reported by Kanemasa, S. et al. Tetrahedron Lett. 1993, 34, 677 [cf. Meyer, R. et al. Liebigs Ann. Chem. 1977, 1183], and liberation of the a -amino group should then provide 229, as a mixture of isomers. Application of the now standard cyclocondensation should complete the synthesis of 231 upon hydrolysis of 230.

A similar sequence should provide an entry into the thiazolines series (235). However, in the case where R^(3b) =H, this material would be prepared by converting 232 to the corresponding mercaptan 233 using the conditions described earlier; the ester in 234 could then be hydrolyzed to afford 235. This reaction sequence would be preferred to avoid use of a presumably unstable thioaldehyde (227 where U=S and R^(3b) =H), see: Takahashi, T. et al. Heterocycles 1993, 36, 1601 and references therein. ##STR62##

Alternative methods for the preparation of these polysubstituted heterocycles employ (Scheme 39) the addition of the anion of isocyanide 236 to an electrophile 227 to provide the heterocycle 237, see: Ito, Y. et al. Tetrahedron Lett. 1989, 30, 4681; Ito, Y. et al. Tetrahedron Lett. 1988, 29, 6321, 235; Ito, Y. et al. Tetrahedron Lett. 1987, 28, 6215; Ito, Y. et al. Tetrahedron 1988, 44, 5253; Meyer, R. et al. Liebigs Ann. Chem. 1977, 1183. The carboxylic ester may be manipulated at this time, however the preferred sequence would implement either an exchange reaction mediated by a transition metal catalyst as reported by Ito, Y. et al. Tetrahedron 1988, 44, 5253 to provide derivatives 238; standard hydrolysis followed by reaction with imidate 211 would also yield 238. Subsequent conversion to the carboxylic acid 239 should proceed smoothly. For cyclic compounds (243) where R²⁰ =H, the preferred sequence would involve the sequential hydrolysis of adduct 240, transformation of the hydroxyl group into a sulfhydryl function, cyclocondensation to thiazoline 242 and finally hydrolysis to afford the desired carboxylic acid 243. ##STR63##

Another noteworthy method (Scheme 40) for the assembly of oxazolines and thiazolines utilizes an appropriate N-acyl-β-hydroxy-α-amino acid (244) which reacts intramolecularly by cyclization of the amide carbonyl onto the hydroxyl group of the amino acid. This transformation may occur upon treatment with triphenylphosphine and an azodicarboxylate, as reported by Wipf, P.; Miller, C. P. Tetrahedron Lett. 1992, 33, 6267, 907 and Galeotti, N. et al. Ibid., 2807, or through the use of diphenyl sulfoxide and triflic anhydride, as demonstrated by Yokokawa, F. et al. Synlett 1992, 153, to generate the requisite ring system; in 245. Hydrolysis of the ester then provides 246. Alternatively, this cyclization may be effected by intramolecular displacement of the corresponding halo derivative (--OH→halogen in 244), which is generated in situ, to provide the oxazoline (245), see: Evans, D. A. et al. J. Org. Chem. 1992, 57, 1961. ##STR64##

The regioisomeric 5-carboxyheterocycles may be synthesized (Scheme 41) by condensation of an appropriate α-functionalized β-amino acid with imidate 211; for an example of this type of cyclization, see: Wolfe, S. et al. Tetrahedron Lett. 1979, 3913. In the event, nucleophilic opening of an a, b--epoxy acid (247) with an inorganic azide such as lithium azide according to Chong, J. M.; Sharpless, K. B. J. Org. Chem. 1985, 50, 1563 should provide 248; the corresponding esters also participate in this reaction, see: Commercon, A. et al. Tetrahedron Lett. 1992, 33, 5185. Reduction should give the requisite α-hydroxy-β-amino acid 249. Alternatively, it may be desirable to prepare 249 from an a--amino acid directly as described by Poss, M. A.; Reid J. A. Tetrahedron Lett. 1992, 33, 1411, by reaction of the appropriate N--BOC compound (250) with 2-furyllithium to provide vicinal amino alcohol (251); manipulation of the furan moiety and deprotection then generates 249. A similar approach using 2-lithiothiazoles may also be useful, see: Dondoni, A.; Perrone, D. Tetrahedron Lett. 1992, 33, 7259. ##STR65##

Completion of the syntheses of the heterocycles should follow precedent. Reaction with of 249 with 211 should provide oxazoline 254 directly. This alcohol may also be used in a sequence described previously to allow for incorporation of sulfur and ultimately provide 250; this mercaptan should lead to thiazoline 251. Additionally, 249 could be employed as a substrate for reaction with a nitrogen based nucleophile, see: Mitsunobu, O. Synthesis 1998, 1 [cf. Cardani, S. et al. Tetrahedron 1988, 44, 5563], to deliver 252 as a precursor for imidazoline 253.

The regioisomeric imiodazolines should be available from other routes as well (Scheme 42). One method would call for hydrolysis of imine 223, discussed earlier in Scheme 37, followed by protection of the newly liberated α-amino group to give 254. Cleavage of the phthaloyl residue and reaction with imidate 211 should provide 255 which is hydrolyzed to 256. An alternative approach calls for reaction of an α-bromo-α,β-unsaturated ester (257) with an amidine (258) [sterically hindered (P is large) materials do not react] to generate 259 in a single step as reported by Marsura, A. et al. Synthesis 1985, 537; hydrolysis of the ester should yield the acid 260. ##STR66##

The several types of inhibitors disclosed in this invention can be broadly classified by their electrophilic functional group A, as defined in Formula (I). The compounds described below, unlike the boron containing peptides, utilize a highly electrophilic carbon atom at A to interact with the active site serine of thrombin. The precursor for the electrophilic carbon inhibitors is the appropriately protected amino acid (261) of Scheme 43. ##STR67##

The preparation of (261) can be found in the general chemical literature, one such reference being the review by Morrison and Mosher (1976). According to Scheme 43 various terminal functional groups are available from (261) : the formamidino-(262), cyanoguanidino-(263), hydroxyguanidino-(264) and guanidino- analogs (265).

The preparation of amidine derivative (267) and phenylguanidines of formula (269) from amino acids (266) and (268), respectively, is shown in Scheme 44. The conditions used to prepare amidines of formula (267) is discussed for (303) of Scheme 53 while the method for formamidinylation of (268) to give (269) is the same as that described to prepare (295) of Scheme 52. ##STR68##

As shown in Scheme 45, appropriately protected derivatives of formulae (261-269), wherein M is an alkyl or benzyl group can be coupled with N,N-disubstituted acid (270) or (271) (wherein M is hydrogen). The X group in compounds of formulae (261) through (269) and (272) in Scheme 45, as well as in compounds illustrated in the Schemes to follow, is a protected version of the terminal functional group X, as defined by Formula (I), unless deprotection is indicated to obtain the final compound of the sequence. ##STR69## It is understood that the protecting group(s) used should compatible with the conditions of the process discussed; a good source for information on protecting group chemistry is Greene and Wuts (1991).

The preparation of the thrombin inhibitors trihalomethyl ketone (274) and α-ketoester (275) are shown in Scheme 46. The coupled ester (272), wherein M is alkyl or benzyl can be converted to the acid (M is hydrogen) by the methodology appropriate for the particular ester functionality as described in Greene and Wuts (1984). The aldehyde (273) can be prepared by selective reduction of the acid (272, M is hydrogen) to the primary alcohol followed by oxidation. ##STR70## To obtain the primary alcohol, the acid can be transformed to the mixed anhydride by condensation of the trialkylammonium salt of the acid with an alkyl- or arylchloroformate in an inert non-polar solvent such as tetrahydrofuran, 1,2-dimethoxyethane or toluene at -78° C. to room temperature. The solution of the resulting mixed anhydride is filtered and reduced to the peptidyl alcohol with an excess of a borohydride reducing agent in a compatible solvent like water or an alcohol at -78° C. to room temperature according to the method of Rodriguez et. al., Tetrahedron Lett. 32, 923 (1991). The peptidyl alcohol can be oxidized to aldehyde (273) without over oxidation by a variety of procedures, as detailed by Hudlicky in Oxidations in Organic Chemistry, American Chemical Society, p. 114 (1991); the preferred methods include Swern oxidation described by Omura and Swern, Tetrahedron 34, 1651 (1978); and the Pfitzner-Moffat oxidation described by Fearon et al. in J. Med. Chem. 30, 1617 (1987). A two step protocol reported by Edwards, Tetrahedron Lett. 33, 4279 (1992) can be used to prepare the trifluoromethyl ketones (274) (J is fluorine) from aldehyde (273). In this procedure a metallated trifluoromethyl anion is generated from an excess of trifluoromethyliodide or -bromide and an active metal such as zinc, magnesium, lithium or cadmium in inert, anhydrous solvents like tetrahydrofuran or N,N-dimethylformamide at temperatures of -100° C. up to the reflux point of the solvent. Alternatively, the metallated trifluoromethyl anion may be generated by the transmetallation of trifluoromethyliodide or -bromide with an organometallic compound such as a Grignard reagent or alkyllithium compound in an inert solvent like tetrahydrofuran, hexane or ether at temperatures ranging from -78° C. up to the reflux point of the selected solvent. Aldehyde (273) can be added to the solution of the metallated trifluoromethyl anion to form the trifluoroethanol derivative at temperatures of -100° C. or higher. To obtain the trifluoromethyl ketone (274) where J is fluoro, the alcohol is oxidized by the Pfitzner-Moffat or Swern procedure. Removal of the protecting group(s) on terminal group X by the appropriate method will provide the thrombin inhibitors of formulae (274).

Trihalomethyl analogs of (274), where J is fluoro can also be prepared from aldehyde (273) by a different method. The trihalomethyl ketones are prepared by treating aldehyde (273) with either the trimethylsilyl trihaloacetate or the potassium or sodium trihaloacetate in a polar solvent such as an alcohol, N,N-dimethylformamide or methylsulfoxide with or without a base such as a trialkyl amine, potassium carbonate or sodium hydroxide at temperatures of -78° C. or higher according to the method of Beaulieu, Tetrahedron Lett. 32, 1031 (1991); Shell Int. Res., European Patent Application EP 16504 ). The resulting α, α, α-trihaloethanol is oxidized and group X can be deprotected as above to give the thrombin inhibitors or formulae (274).

The α-ketoester thrombin inhibitors, exemplified by (276), are prepared according to a route disclosed by Iwanowicz et. al. in Bioorgan. Med. Chem. Lett. 12, 1607 (1992). The tris(ethylthio)methyl anion is added to the peptidyl aldehyde (273) in a solvent such as tetrahydrofuran, 1,2-dimethoxyethane or toluene at -100° C. or higher to give the alcohol (275). The α-hydroxyl ester is generated from (275) by treatment with a mixture of mercuric salts, such as mercuric chloride and mercuric oxide, in an alcohol or water. Swern or Pfitzner-Moffat oxidation of the s-hydroxyl ester followed by the deprotection of substituent X protecting group provides thrombin inhibitors of formula (276).

Another method for the preparation of compound (276) substitutes a 1-lithio-1-alkoxyethene or 1-magnesio-1-alkoxyethene for the tris(ethylthio)methyl anion of Scheme 15 in an addition reaction with peptidyl aldehyde (273). There can be obtained an adduct analogus to the tris(ethylthio)hydroxyethyl compound (275) when excess 1-magnesio- or 1-1-lithio-1-alkoxyethene anion is stirred at temperatures ranging from -100 ° C. to ambient temperature with (273) in anhydrous solvents such as diethyl ether or tetrahydrofuran. This alkoxyolefin product may then be transformed to (276) by oxidative cleavage with reagents such as ozone or periodate in an inert solvent such as a halohydrocarbon, lower alkyl ketone, an alcohol or water at temperatures ranging from -100° C. to ambient temperature, followed by oxidation of the intervening α-hydroxyester and deprotection as described above.

The preparation of the α,α-dihalomethylketone thrombin inhibitors of this invention is outlined in Scheme 47. ##STR71##

The α,α-dihalomethylketone (279), where J is fluoro can be prepared from the aldehyde (273) by selective reaction of the aldehyde with the anion of the corresponding dihalomethane. The metallated dihalomethane anion is generated from one equivalent each of a strong hindered base, such as lithium tetramethylpiperidide or tertbutyllithium, and the selected dihalomethane in an anhydrous, inert solvent like tetrahydrofuran or 1,2-dimethoxyethane at -100° C. or higher according to the method of Taguchi et. al. Bull. Chem. Soc. Jpn., 50, 1588 (1977). The metallated dihalomethane anion can be added to the aldehyde (273) at -100° C. or higher. Alternatively, the dihalomethane anion is generated from a dihalomethyl(trimethyl)silane and an anhydrous fluoride ion source such as tris(diethylamino)sulfonium difluoromethyl silicate in an inert solvent like benzene, acetonitrile or tetrahydrofuran at -78° C. or higher, then (273) can be added to give dihaloethanol (278) according to the method of Fujita and Hiyama, J. Am. Chem. Soc. 107, 4085 (1985). The resulting dihaloethanol can be oxidized to ketone (279) by the Swern or Pfitzner-Moffat procedure. Removal of the protecting group(s) on substituent X of (279) gives the α,α-dihalomethylketone thrombin inhibitors.

α-Halomethylketone thrombin inhibitors can be prepared by the process illustrated in Scheme 48. The acid chloride (281) can be prepared from acid (272), wherein M is hydrogen or its trialkylammonium, sodium or potassium salt with a chlorinating agent such as thionyl chloride, oxalyl chloride or dichloromethylmethyl ether in a solvent like tetrahydrofuran or dichloromethane with or without a catalytic amount of N,N-dimethylformamide at -78° C. or higher. Alternatively, the mixed anhydride of (272) may be prepared as described for (272) in Scheme 46. Compound (281) or the mixed anhydride of (272) can be treated with an ether solution of diazomethane and either anhydrous hydrogen fluoride or hydrogen chloride gas according to that described by McPhee and Klingsbury, Org. Synth. Coll. III, 119 (1955); or hydrogen bromide according to the method Miescher and Kaji, Helv. Chim. Acta. 24, 1471 (1941). ##STR72##

Selection of the hydrogen fluoride gas will give the α-fluoromethylketone analog, (282) wherein J is fluoro; and hydrogen chloride gas gives the α-chloromethylketone analog (282) wherein J is chloro. Deprotection of X gives the corresponding thrombin inhibitors of (282).

The general preparative route for the α,β-diketoester, -amide and -ketone thrombin inhibitors of this invention is exemplified in Scheme 49. Compound (281) or the mixed anhydride of (272) can be reacted with a Wittig reagent such as methyl (triphenylphosphoranylidene)acetate in a solvent like tetrahydrofuran or acetonitrile at temperatures ranging from 0° C. to the reflux point of the solvent to give (284). Oxidative cleavage of the phosphoranylidene (284) with an oxidizing agent like ozone or OXONE™ in an inert solvent such as tetrahydrofuran, dichloromethane or water at temperatures of -78° C. or higher gives the vicinal tricarbonyl compound (285), analogous to that described by Wasserman and Vu, Tetrahedron Lett. 31, 5205 (1990). Cleavage of the protecting group can provide thrombin inhibitors of formula (285). ##STR73##

The preparative routes for the synthesis of the α-mono- and α,α-dihalo-β-ketoester -amide and ketone thrombin inhibitors of this invention are summarized in Scheme 50. The exemplified β-ketoester (287) is available from the acid derivative (272). The acid (272) can be treated with carbonyl diimidazole in an inert solvent such as tetrahydrofuran or dichloromethane at 0° C. or higher to form the acyl imidazole. This acyl imidazole, or the mixed anhydride of (272), can be further reacted with lithioethylacetate in solvents such as 1,2-dimethoxyethane or tetrahydrofuran/hexane at temperatures ranging from -100° C. to ambient temperature, according to the method of Dow, J. Org. Chem. 55, 386 (1990) to give β-ketoester (287). ##STR74## Compound (287) serves as a substrate for both mono- and dihalogenation. The α-monochloro analog of (288), where J is each chlorine and hydrogen, can be prepared by controlled halogenation reactions with reagents like N-chlorosuccinimide or thionyl chloride in an inert halogenated solvent and at temperatures ranging from -20° C. to the reflux point of the selected solvent according to the methods of Uhle, J. Am. Chem. Soc. 83, 1460 (1961); and DeKimpe et. al., Synthesis 2, 188 (1987). The α,α-dihalo analog (289) where J is chloro is available from halogenation with molecular chlorine in a halogenated solvent at temperatures of -20° C. or higher according to the method of Bigelow and Hanslick, Org. Syn. Coll. II, 244 (1943). Reagents such as N-fluorobis[(trifluoromethyl)sulfonyl]imide are useful for the preparation of mono- and difluoro analogs (288) and (289) by reacting the appropriate stoichiometry of this reagent with (287) in a halogenated solvent at temperatures of -78° C. or higher according to the method of Resnati and DesMarteau, J. Org. Chem. 56, 4925 (1991). Deprotection of substituent X of the halogenation products (288) and (289) can provide the corresponding thrombin inhibitors.

Compounds of formula (287) also serves as a substrate for the preparation of tricarbonyl derivatives such as (285) (Scheme 49). Condensation of (287) with an aldehyde, such as benzaldehyde, gives an β-ene-β,γ-dione. This ene-dione can be oxidatively cleaved with reagents like ozone or periodate to give tricarbonyl analog (285).

The preparation of the mono- and dihalomethylketone thrombin inhibitors is outlined in Scheme 51. The intermediates formed in the preparation of the α-mono- and α,α-dihalo-β-ketoester thrombin inhibitors of Scheme 49 can be used in these preparations. ##STR75## The decarboxylation of these halogenation products, (288) and (289), can be effected by saponification of the ester with mild aqueous base such as potassium carbonate or sodium hydroxide in water miscible solvents like an alcohol, tetrahydrofuran or N,N-dimethylformamide, followed by adjusting the pH to a range of 4 to 6. This mixture can be either stirred at ambient temperatures or heated at various temperatures up to the reflux point of the solvent chosen until the formation of (279) or (282) is complete and is similar to that reported in Matsuda et. al., Tetrahedron Lett. 30, 4259 (1989). Removal of protecting group(s) can provide thrombin inhibitors corresponding to (279) or (282).

A process for the preparation of the boropeptide thrombin inhibitors of this invention from intermediates (291) and (292) is disclosed in Scheme 52. Compound (291) serves as a starting point for isothiouronium thrombin inhibitors (296) and (297). The boronic ester (296) is prepared by stirring a solution of (291) and thiourea in an inert polar solvent, such as an alcohol or N,N-dimethylformamide, at temperatures ranging from ambient to the reflux temperature of the selected solvent. It is understood that a boronic acid ester like compound (296) is an effective thrombin inhibitor, however, it may be transformed to the corresponding free boronic acid (297) without a loss of biological activity. Compound (297) is derived from the boron ester (296) by transesterification under equilibrium conditions. ##STR76## Thus stirring ester (296) with an excess of an alkyl- or aryl boric acid in a biphasic mixture of neutral or acidic water and an immiscible solvent, such as ethyl ether or toluene, gives (297) after several hours at ambient temperature. The conditions generally preferred use 5 to 10 equivalents of phenylboric acid in ethyl ether/water at neutral pH. Thrombin inhibitors (293) to (299) are obtained by reduction of an azide-intermediate prepared from (291) or (292). The azide intermediate is prepared by heating either (291) or (292) with an inorganic azide, such as sodium or potassium azide, in an anhydrous polar aprotic solvent, such as acetone, dimethylformamide or methyl sulfoxide at temperatures ranging from ambient to 130° C. Alternatively, phase transfer conditions may be employed to prepare the azide intermediate from (291) or (292). For example, a tetraalkylammonium azide in a non-polar aprotic solvent, such as tetrahydrofuran or toluene, or a crown ether and inorganic azide in biphasic mixtures of water and an immiscible solvent, such as benzene, toluene or xylene, can be stirred at room temperature or heated up to the reflux point of the selected solvent. The primary amines (293) and (294) are most conveniently obtained from the catalytic hydrogenation of the azide in an inert solvent, such as an alcohol, ethyl acetate or tetrahydrofuran with a transition metal catalyst such as platinum or palladium on carbon under an atmosphere of hydrogen gas. A variety of alternative methods are also useful and can be found in the monograph by Hudlicky (1984, pp. 76). The acid salt of the resulting amines (293) and (294) may be formed by the addition of one equivalent of the desired acid to the hydrogenation mixture. Phenylboric acid mediated hydrolysis of esters (293) and (294) gives the free boronic acid thrombin inhibitors (298) and (299), compounds of formula (I) of the invention.

Compounds containing a primary guanidine or N-alkyl guanidine functionality may be prepared by the alternative process outlined in Scheme 52. As illustrated with primary amine (293), the transformation to (295) is effected with a guanidinylation agent, such as an S-alkyl thiourea, aminoiminomethane sulfonic acid reported by Miller and Bischoff Synthesis 9, 777 (1986), cyanamide reported by Kettner et al. (1990) or their N-alkyl derivatives. This mixture is stirred at room temperature or higher with a base, such as potassium carbonate, triethylamine or N,N-dimethylaminopyridine in an inert solvent like water, alcohol, N,N-dimethylformamide or acetone. The guanidine boronic acid esters (295) can be deesterified to give the corresponding boronic acid (300) by the phenylboric acid procedure described above.

According to Scheme 53, the bromide (292) is converted to the corresponding alkylnitrile (302) upon exposure to the cyanide anion under a variety of conditions. ##STR77## Effective methods include the use of potassium or sodium cyanides in polar aprotic solvents, such as N,N-dimethylformamide, methylsulfoxide, acetone or ethylmethyl ketone, at temperatures ranging from ambient up to the reflux point of the selected solvent. More useful, however, are conditions employing phase transfer agents such as tetrabutylammonium cyanide in a nonpolar aprotic solvent such as tetrahydrofuran or toluene, or a biphasic mixture of a crown ether and an inorganic cyanide in water with an immiscible solvent like benzene, toluene or xylene. These mixtures can be stirred at ambient temperature or heated up to the reflux temperature of the selected solvent. An amidine like (303) is prepared by first treating nitrile (302) with a saturated solution of a mineral acid such as hydrogen chloride in an alcohol solvent at room temperature or lower. The intermediate O-alkylimidate can be exposed to ammonia, or a primary or secondary amine under anhydrous conditions with or without an inert solvent. As illustrated in Scheme 5, compound (303) is produced by treating the O-alkylimidate formed from (302) with neat anhydrous ammonia at reflux. The free boronic acid (304) is obtained by transesterification of (303) with phenylboric acid in a mixture of water and diethyl ether.

EXAMPLE 1 N¹ -(4-Phenylbenzoyl)boroarginine (+)-Pinanediol, Bisulfite

Part A: (+)-Pinanediol 4-bromo-1(R)-(4-phenylbenzoyl) aminobutane-1-boronate. To a solution of (+)-pinanediol 4-bromo-1(R)-aminobutane-1-boronate hydrochloride (5.00 g, 13.6 mmol) in dichloromethane (50 mL) at 0° C. was added 4-phenylbenzoyl chloride (4.97 g, 22.9 mmol) followed by N-methylmorpholine (4 mL, 36 mmol). After 1 hour, the cooling bath was removed and the mixture stirred at room temperature for 2 hours. The mixture was then diluted with ethyl acetate and washed with 0.1M hydrochloric acid, saturated sodium bicarbonate and saturated sodium chloride. The organic phase was dried over anhydrous magnesium sulfate, filtered and the filtrate concentrated in vacuo to afford 3.37 g (48%) of the desired amide, mass spectrum: (M+H)⁺ =510/512; ¹ H NMR (300 MHz, CDCl₃) d7.9 (2H, d, J=8.3), 7.84 (1H, bs), 7.6 (2H, d, J=8.3), 7.44 (5H, m), 4.37 (1H, m), 3.41 (1H, t, J=6.9), 2.0 (10H, m) 1.49 (3H, s), 1.38 (1H, m), 1.29 (3H, s), 0.91 (3H, s).

Part B: (+)-Pinanediol 4-azido-1(R)-(4-phenylbenzoyl) aminobutane-1-boronate. To a solution of (+)-pinanediol 4-bromo-1(R)-(4-phenylbenzoyl)aminobutane-1-boronate (3.37 g, 6.60 mmol) in dimethylformamide (6 mL) was added sodium azide (547 mg, 8.41 mmol). The resulting mixture was heated at 70° C. for 2 hours, cooled to room temperature, and diluted with ethyl acetate. The mixture was then washed with water, saturated sodium chloride and dried over anhydrous magnesium sulfate. Filtration, followed by concentration of the filtrate in vacuo gave 3.04 g (97%) of the desired azide, mass spectrum: (M+H)⁺ =473; ¹ H NMR (300 MHz, CDCl₃) d7.89 (2H, d, J=8.3), 7.75 (1H, bs), 7.3 (7H, m), 4.32 (1H, m), 3.32 (1H, m), 2.0 (10H, m) 1.48 (3H, s), 1.3 (4H, m), 0.9 (3H, s).

Part C: N¹ -(4-Phenylbenzoyl)boroornithine (+)-pinanediol, hydrochloride. To a solution of (+)-pinanediol 4-azido-1(R)-(4-phenylbenzoyl)aminobutane-1-boronate (3.04 g, 6.44 mmol) in methanol (30 mL) was added Pearlman's catalyst (Pd(OH)₂ /C, 200 mg) and 1M hydrochloric acid (6.5 mL, 6.5 mmol). The mixture was placed on a Parr apparatus and hydrogenated at 50 psi for 3 hours. The mixture was filtered using Celite™, washed with methanol and the filtrate concentrated in vacuo. The resulting amorphous solid was dissolved in water and washed with ether. The aqueous phase was then concentrated in vacuo and crystallized from ethyl acetate-hexanes, giving 1.52 g (49%) of the desired amine hydrochloride, mass spectrum: (M+H)⁺ =447; mp: 157°-170 ° C.; ¹ H NMR (400 MHz, CDCl₃ /DMSO-d₆) d9.88 (1H, bs), 8.18, (2H, d, J=8.3), 8.13 (3H, bs), 7.68 (2H, d, J=8.3), 7.61 (2H, d J=7.0), 7.45 (2H, d, J=7.0), 7.37 (1H, d, J=7.30), 4.20 (1H, d, J=6.3), 2.99 (1H, m), 2.87 (2H, m), 2.31 (1H, m), 2.13 (1H, m), 1.84 (7H, m), 1.56 (1H, d, J=10.0), 1.42 (3H, s), 1.29 (3H, s), 0.89 (3H, s).

Part D: N¹ -(4-Phenylbenzoyl)boroarginine (+)-pinanediol, bisulfite. To a solution of N¹ -(4-phenylbenzoyl)boroornithine (+)-pinanediol, hydrochloride (80 mg, 0.17 mmol) in ethanol (2 mL) was added 4-dimethylaminopyridine (40 mg, 0.33 mmol). After 15 minutes, aminoiminomethanesulfonic acid (40 m g, 0.32 mmol) was added and the resulting mixture heated at reflux for 3 hours. After cooling to room temperature, the mixture was filtered and the filtrate concentrated in vacuo. The residue was dissolved in chloroform and washed with 0.1M hydrochloric acid, water and dried over anhydrous magnesium sulfate. Filtration, followed by concentration of the filtrate in vacuo afforded 73 mg (84%) of the desired guanidine, mass spectrum: (M+H)⁺ =489; ¹ H NMR (400 MHz, CDCl₃, 60° C.) d9.48 (1H, bs), 8.10 (2H, d, J=8.1), 8.07 (1H, bs), 7.75 (1H, bs), 7.54 (2H, d, J=8.3), 7.48 (2H, d, J=7.0), 7.35 (3H, m), 7.06 (4H, bs), 4.19 (1H, bd, J=8.3), 3.1 (2H, m), 2.84 (1H, m), 2.29 (1H, m), 2.12 (1H, m), 1.96 (1H, m), 1.75 (6H, m), 1.47 (1H, d, J=10.2), 1.40 (3H, s), 1.24 (3H, s), 0.83 (3H, s).

EXAMPLE 34 (+)-Pinanediol 4-(Formamidino)thio-1(R)-(4-phenylbenzoyl) aminobutane-1-boronate, Hydrobromide

(+)-pinanediol 4-(formamidino)thio-1(R)-(4-phenylbenzoyl) aminobutane-1-boronate, hydrobromide. To a solution of (+)-pinanediol 4-bromo-1(R)-(4-phenylbenzoyl) aminobutane-1-boronate (200 mg, 0.392 mmol) in methanol (3 mL) was added thiourea (120 mg, 1.58 mmol). The reaction was stirred at room temperature for 3 days. The mixture was concentrated in vacuo, the residue dissolved in water and washed with ether. Concentration of the aqueous portion afforded 80 mg (35%) of the desired isothiourea, mass spectrum: (M+H)⁺ =506; ¹ H NMR (300 MHz, CDCl₃) d8.15 (2H, d, J=8.4), 7.61 (2H, d, J=8.4), 7.52 (2H, m), 7.38 (3H, m), 6.47 (1H, bs), 4.23 (1H, dd, J=6.6, 1.9), 3.24 (1H, m), 3.14, (1H, m), 2.96, (1H, m), 2.32 (1H, m), 2.15 (1H, m), 1.99 (1H, m), 1.78 (6H, m), 1.48 (1H, d, J=10.1), 1.42 (3H, s), 1.27 (3H, s), 0.86 (3H, s). ##STR78##

EXAMPLE 898

R--N¹ -(3-Cyanomethyl-5-phenylmethyl-1,2,4-traizol-1-yl) acetyl-borolysine, (+)-pinanediol ester, hydrochloride; X=--CH₂ NH₂, R¹³ =--CH₂ Ph, R¹⁴ =--CH₂ CN, Y¹,Y² =(+)-pin. ##STR79##

Part A. Ethyl benzylimidate, hydrochloride.

HCl gas (17.1 g, 469 mmol, 1.1 eq) was slowly bubbled into a solution of phenylacetonitrile (50.00 g, 427 mmol, 1 eq) in ethanol (27.6 mL, 469 mmol, 1.1 eq) at 0° C. The reaction was put into the refrigerator over the weekend. After warming to room temperature, ether (300 mL) was added to the reaction mixture which had solidified and the contents were vigorously stirred at 0° C. to pulverize the mixture. The solid material was filtered while cold under an inert atmosphere and the filter cake rinsed with some more ether. The product was dried under high vacuum to yield 60.0 g (mp 94.0°-95.0° C.) of a white solid. A second crop yielded 20.98 g (96.0°-97.5° C). ##STR80##

Part B. 3-Cyanomethyl-5-phenylmethyl-1,2,4-triazole.

The imidate from part A (14.92 g, 91 mmol, 1 eq) was dissolved in ethanol (250 mL) and cooled to 0° C. under an inert atmosphere. Cyanoacetohydrazide (9.06 g, 91 mmol, 1 eq) dissolved as best possible in warm ethanol was added, and the resultant mixture stirred at room temperature overnight. The mixture was filtered, and the filtrate concentrated to yield a gummy orange solid. Trituration from hexanes yielded 19.72 g of solid product acylamidrazone (MS detects (M+H)⁺ =216). This intermediate was heated neat (oil bath) at 170° C. under an inert atmosphere for 0.5 h to crack out water. The product was cooled to room temperature and dissolved in ethyl acetate. The solvent was dried (MgSO4) and stripped to yield 11.89 g of an orange solid. Flash chromatography over silica gel in solvent systems consisting of 3:1 pentane/ethyl acetate to 100% ethyl acetate to 4:1 chloroform/methanol yielded 6.76 g (38%) of a light pink solid product; m.p.=140.0°-142.5° C. NMR (DMSO-d₆) ∂14.00-13.60 (bs, 1H); 7.40-7.10 (m, 5H); 4.08 (s, 2H); 4.05 (s, 2H). MS: (M+H)⁺ =199. ##STR81##

Part C. Ethyl (3-cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetate.

The compound from part B (3.36 g, 17 mmol, 1 eq) was added portionwise to a mixture of DMF and 50% NaH (0.81 g, 17 mmol, 1 eq) at 25° C. After H₂ evolution had ceased, the mixture was heated a little with a heat gun to ensure complete deprotonation. The mixture was cooled to 0° C. and ethyl bromoacetate (1.88 mL, 17 mmol, 1 eq) was added. The reaction was allowed to warm to room temperature and was stirred overnight. Ethyl acetate was added and the mixture washed with water (5×) to remove the DMF. The organic layer was dried (MgSO₄) and stripped to yield 6.10 g of a reddish oil. Flash chromatography in 3:1 hexanes/ethyl acetate to 1:1 hexanes/ethyl acetate yielded 2.93 g of an amber oil which consisted of a 4:1 mixture of regioisomers as determined by NMR with the major isomer being depicted above. NMR (major isomer) (CDCl₃) ∂7.40-7.20 (m, 5H); 4.68 (s, 2H); 4.25-4.05 (m, 4H); 3.84 (s, 2H); 1.23 (t, 3H, J=7 Hz). ##STR82##

Part D. (3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetic acid.

The product of part C (1.00 g, 3.52 mmol, 1 eq), 1.000N NaOH (7.03 mL, 7.03 mmol, 2 eq) and methanol (10 mL) were mixed and stirred at room temperature. After 24 h, the methanol was stripped and the aqueous mixture washed with ether (2×). The aqueous layer was then acidified with conc. HCl and extracted with ethyl acetate (3×). The organic layers were combined, dried (MgSO₄) and stripped to yield 0.66 g of an off-white glass. MS (M+H)⁺ =257. ##STR83##

Part E. (+)-pinanediol 5-bromo-1(R)-((3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetamido)pentane-1-boronate.

N-methylmorpholine (0.42 mL, 3.86 mmol, 1.5 eq) was added to a solution of the product in part D (0.66 g, 2.58 mmol, 1 eq) in THF at 25° C. The mixture was cooled to -20° C. and isobutylchloroformate (0.50 mL, 3.86 mmol, 1.5 eq) in THF was added dropwise. In a separate flask, pinanediol 5-bromo-1-R-aminopentane-1-boronate hydrochloride (0.98 g, 2.58 mmol, 1 eq) was dissolved in CHCl₃ and cooled to -78° C. Triethylamine (0.36 mL, 2.58 mmol, 1 eq) was then added and the mixture syringed immediately into the reaction flask with the mixed anhydride. The reaction was allowed then to warm to room temperature overnight. The next day, the precipitate was filtered off and the solids were rinsed with THF. The filtrate was stripped to yield 410 mg of a white oil. Flash chromatography over silica gel in solvent systems consisting of 3:1 pentane/ethyl acetate to 100% ethyl acetate to 4:1 chloroform/methanol yielded 300 m g of a clear, colorless viscous oil and only one regioisomer by NMR. MS (M+H)⁺ =633 and 635. NMR (CDCl₃) ∂7.40-7.10 (m, 5H); 6.13 (d, 1H, J=6 Hz); 4.62 (s, 2H); 4.40-4.20 (m, 1H); 4.17 (s, 2H); 3.86 (s, 1H); 3.50-3.20 (m, 3H); 2.40-2.10 (m, 2H); 2.10-1.75 (m, 4H); 1.75-1.10 (m, 13 H); 0.83 (s, 3H). ##STR84##

Part F. (+)-pinanediol 5-azido-1(R)-((3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetamido)pentane-1-boronate.

The product from Part E (300 mg, 0.52 mmol, 1 eq), sodium azide (1.03 mmol, 2 eq), and DMSO (5 mL) were mixed and stirred at room temperature under an inert atmosphere for 24 h. Ethyl acetate was added and the mixture rinsed with water (5×). The ethyl acetate layer was dried (MgSO₄) and stripped to yield 256 mg of a light amber oil. IR (neat) 2096 cm-1. NMR (CDCl3) ∂7.40-7.10 (m, 5H); 6.15 (d, 1H, J=6 Hz); 4.62 (s, 2H); 4.40-4.20 (d of d, 1H, J=7, 2 Hz); 4.20-4.10 (m, 2H); 3.85 (s, 2H); 3.40-3.10 (m, 3H); 2.50-1.40 (m, 9H); 1.40-1.00 (m, 9 H); 0.84 (s, 3H). ##STR85##

Part G. (+)-Pinanediol 5-amino-1(R)-((3-Cyanomethyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetamido)pentane-1-boronate, hydrochloride salt.

The product from Part F (250 mg, 0.46 mmol, 1 eq) and triphenylphosphine (157 mg, 0.6 mmol, 1.3 eq) and THF (5 mL) were mixed and stirred at room temperature. After 1 h, water (11 μM, 0.6 mmol, 1.3 eq) was added and the mixture stirred overnight. After 24 h, the reaction was not finished, and thus 1.3 eq more equivalents of water were added and the reaction stirred for another 24 h. The reaction was now complete and 1 equivalent of 1.000N HCl was added. The reaction was then stripped and water was added and the reaction again stripped. Ethyl ether was added and the mixture stripped once more. The residue was dried under high vacuum to yield 138 mg of a white glass. MS detects (M+H)⁺ =519 and 385 (minus pinanediol). Mass calculated for C₂₈ H₄₀ BN₆ O₃ : 519.3255. Found: 519.3274. NMR shows a 1:1 mixture of pinanediol ester and free boronic acid. ##STR86##

EXAMPLE 908

R-N¹ -(3-(1H-tetrazol-5-yl)methyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetyl-borolysine, (+)-pinanediol ester, hydrochloride; X=--CH₂ NH₂, R¹³ =CH₂ ph, R¹⁴ =--CH₂ --(CN₄ H), Y¹,Y² =(+)-pin. ##STR87##

Part A. Ethyl (3-(N-triphenylmethyl)-1H-tetrazol-5-yl) methyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetate

The product from Example 360, part C (1.83 g, 6.44 mmol, 1 eq), tributyltin chloride (1.75 mL, 6.44 mmol, 1 eq), sodium azide (0.42 g, 6.44 mmol, 1 eq), and xylenes (15 mL) were mixed and refluxed for 24 h under an inert atmosphere. The mixture was cooled to room temperature and pyridine was then added (0.57 mL, 7.08 mmol, 1.1 eq) followed after 0.5 h by trityl chloride (1.97 g, 7.08 mmol, 1.1 eq). The following day, the reaction was worked up by adding ethyl ether and rinsing the mixture with water (3×). The ether layer was dried (MgSO4), and stripped to yield 5.66 g of an amber oil. Flash chromatography in 3:1 pentane/ethyl acetate to 100% ethyl acetate over silica gel yielded 1.33 g of an amber oil which eventually crystallized. MS detects (M+H)⁺ =570 and 328 (M+H--CPh₃)⁺. ##STR88##

Part B. (3-(N-Triphenylmethyl)-1H-tetrazol-5-yl)methyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetic acid.

The product from part A (200 mg, 0.35 mmol, 1 eq), 1.000N NaOH (0.39 mL, 0.39 mmol, 1.1 eq) and THF (5 mL) were mixed and stirred at room temperature under an inert atmosphere for 24 h. The reaction was not finished and thus 0.5 eq more of 1.000N NaOH were added and stirred overnight. Water was then added and the pH adjusted to 5 with 1N HCl. The mixture was stripped to dryness. The residue was stirred in ethyl acetate. Some solids were filtered and the filtrate was stripped to yield 190 mg of a white glass. NMR (CDCl₃) ∂7.40-7.15 (m, 12H); 7.15-7.00 (m, 8H); 4.55 (s, 2); 4.40 (s, 2H); 4.10 (s, 2H). ##STR89##

Part C. (+)-Pinanediol 5-azido-1(R)-((3-((N-triphenylmethyl)-1H-tetrazol-5-ylmethyl)-5-phenylmethyl-1,2,4-triazol-1-yl)acetamido)pentane-1-boronate.

The compound in part B was converted to the corresponding azidoboronic acid pinanediol ester by the methods disclosed in example 360, parts E and F. IR (neat) 2095 cm⁻¹. NMR (CDCl₃) ∂7.45-7.20 (m, 12H); 7.17 (d, 2H, J=7 Hz); 7.12 (d, 6H, J=7 Hz); 6.34 (d, 1H, J=6 Hz); 4.60 (s, 2H); 4.42 (s, 2H); 4.27 (d, 1H, J=7 Hz); 3.13 (t, 2H, J=2 Hz); 3.06 (q, 1H, J=7 Hz); 2.40-2.10 (m, 2H); 2.01 (t, 1H, J=6 Hz); 1.95-1.70 (m, 2H); 1.60-1.40 (m, 4H); 1.37 (s, 3H); 1.35-1.20 (m, 5H); 1.16 (d, 1H, J=11 Hz); 0.82 (s, 3H). MS detects (M+H)⁺ =830 and (M+H-CPh₃)⁺ =588. ##STR90##

Part D. R-N¹ -(3-(1H-tetrazol-5-yl)methyl-5-phenylmethyl-1,2,4-triazol-1-yl)acetyl-borolysine, (+)-pinanediol ester, hydrochloride.

The product form part C (135 mg, 0.16 mmol, 1 eq), 10% Pd on carbon (25 mg), chloroform (39 μL, 0.49 mmol, 3 eq) and methanol (5 mL) were mixed and stirred under hydrogen under balloon pressure for 24 h at room temperature. The mixture was filtered through a Celite® cake rinsing the cake well with methanol afterwards. The filtrate was stripped to yield an off-white glass. This glass was triturated with ethyl ether to yield after drying 50 mg of an of-white solid. Mass calcd. for C₂₈ H₄₁ BN₉ O₃ : 562.3425. Found: 562.3413. NMR (DMSO-d₆) ∂8.75-8.50 (m, 1H); 7.40-7.10 (m, 5H); 4.87 (bs, 2H); 4.30-4.00 (m, 5H); 2.96-2.60 (m, 3H); 2.40-2.00 (m, 2H); 1.91 (t, 1H, J=6 Hz); 1.90-1.75 (m, 1H); 1.75-1.10 (m, 14 H); 0.80 (s, 3H). ##STR91##

EXAMPLE 3458.

R-N¹ -((2-phenyl-4-methylpyrimidin-5-yl) carbonyl)borolysine, (+)-pinanediol ester, hydrochloride; X=--CH₂ NH₂, R¹³ =--Ph, R¹⁴ =--CH₃, R¹⁵ =H, Y¹,Y² =(+)-pin. ##STR92##

Part A. 2-Phenyl-4-methylpyrimidin-5-carboxylic acid.

The above compound was synthesized by the procedure of P. Schenone, L. Sansebastiano, L. Mosti J. Heterocyclic Chem. 1990, 27, 302 which is generally applicable to a wide variety of pyrimidine-5-carboxylic acids.

Part B. R-N¹ -((2-phenyl-4-methylpyrimidin-5-yl) carbonyl)borolysine, (+)-pinanediol ester, hydrochloride.

The product was obtained using the procedures described in example 360, parts E and F and example 361, part D followed by prepatory TLC in 4:1 chloroform/methanol. (M+H)⁺ =477. NMR (DMSO-d₆) ∂8.86 (s, 1H); 8.50-8.30 (m, 2H); 7.70-7.40 (m, 3H); 4.25 (d, 1H, J=7 Hz); 2.90-2.70 (m, 3H); 2.64 (s, 3H); 2.40-1.00 (m, 15H); 0.84 (s, 3H). ##STR93##

EXAMPLE 3538

R-N¹ -((2-phenyl-4-methylpyrimidin-5-yl) carbonyl)boroarginine, (+)-pinanediol ester, hydrochloride; X=--NH(C═NH)NH₂, R¹³ =--Ph, R¹⁴ =--CH₃, R¹⁵ =H, Y¹,Y² =(+)-pin. ##STR94##

Part A. R-N¹ -((2-phenyl-4-methylpyrimidin-5-yl)carbonyl) boroornithine, (+)-pinanediol ester, hydrochloride.

The above intermediate was synthesized by the procedures described for example 361 using the appropriate starting materials.

Part B. R-N¹ -((2-phenyl-4-methylpyrimidin-5-yl) carbonyl)boroarginine, (+)-pinanediol ester, hydrochloride.

The product form part A (500 mg, 1 mmol, 1 eq), formamidinesulfonic acid (224 mg, 1.8 mmol, 2 eq), 4-(N,N-dimethylamino) pyridine (220 mg, 1.8 mmol, 2 eq, and ethanol (20 mL) were mixed and refluxed under an inert atmosphere for 5 hours. Some solid material was filtered and the filtrate was stripped to yield a yellow glass. The glass was taken up in chloroform/0.1N HCl. Solids precipitated. These were filtered and dried to yield 144 mg of product as a white powder: mp 132° C. (dec.). (M+H)⁺ =505.

Mass calcd. for C₂₇ H₃₈ BN₆ O₃ : 505.3086. Found: 505.3098. NMR (DMSO-d₆) ∂8.89 (s, 1H); 8.60-8.40 (m, 2H); 8.05-7.80 (m, 1H); 7.65-7.40 (m, 3H); 7.40-6.80 (m, 3H); 4.19 (d, 1H, J=7 HZ); 3.60-3.20 (m, 3H); 2.85-2.40 (m, 4H); 2.40-1.95 (m, 1H); 1.95-1.00 (m, 16H); 0.80 (t, 3H). ##STR95##

EXAMPLE 5926. N¹ -[(4R)-2-(2-Phenyl)ethyl-Thiazoline-4-Carboxy]-R-borothioarginine-(+)-pinanediol ester

Part A. (4R)-2-(2-phenyl)ethyl-thiazoline-4-carboxylic acid ethyl ester.

Cysteine ethyl ester hydrochloride (950 mg, 5.10 mmol) was added to a solution of ethyl (2-phenyl)ethylimidate (900 mg, 5.10 mmol) [prepared by the method of North, M.; Pattenden, G. Tetrahedron 1990, 46, 8267] in EtOH (20 mL) at room temperature. The reaction mixture was stirred for 16 h and concentrated under reduced pressure. The residue was partitioned between H₂ O (ca. 50 mL) and EtOAc (ca. 100 mL) and the layers were separated; the aqueous phase was extracted with EtOAc (1×20 mL). The combined organic layers were washed with saturated aqueous NaCl (1×50 mL), dried (Na₂ SO₄), and concentrated under reduced pressure to give an oil which was purified by flash chromatography, elution with 3:1 hexanes--EtOAc, to afford 885 mg (66%) of the title compound as a colorless oil. ¹ H NMR (300 MHz, CDCl₃) δ7.23 (comp, 5H), 5.05 (dd, 1H, J=9.5, 9.1 Hz), 4.27 (dq, 2H, J=7.0, 1.8 Hz), 3.55 (m, 2H), 2.97 (m, 2H), 2.86 (m, 2H), 1.32 (t, 3H, J=7.0 Hz); LRMS 264 (M+1, base).

Part B. (4R )-2-(2-phenyl)ethyl-thiazoline-4-carboxylic acid.

A solution of lithium hydroxide monohydrate (96 mg, 2.28 mmol) in H₂ O (2 mL) was added to a solution of (4R)-2-(2-phenyl)ethyl-thiazoline-4-carboxylic acid ethyl ester (400 mg, 1.52 mmol) in THF (8 mL) and MeOH (5 mL). The reaction mixture was stirred at room temperature for 1 h at which time 2M aqueous HCl was added until pH=2 and the aqueous phase was extracted with EtOAc (2×30 mL). The combined organic layers were washed with saturated aqueous NaCl (1×20 mL), dried (MgSO₄), and concentrated under reduced pressure to give 340 mg (95%) of the title compound as an oil. ¹ H NMR (300 MHz, CDCl₃) δ7.22 (comp, 5H), 6.86 (br s, 1H), 5.14 (dd, 1H, J=9.5, 9.1 Hz), 3.64 (m, 2H), 2.96 (comp, 4H); LRMS 236 (M+1, base).

Part C. (1R)-4-Bromo-1-[(4R)-2-(2-Phenyl)ethyl-thiazoline-4-carbox]amido-1-boronic acid-(+)-pianediol ester,

A solution of (4R)-2-(2-phenyl)ethyl-thiazoline-4-carboxylic acid (335 mg, 1.43 mmol) and 4-methylmorpholine (0.47 mL, 4.28 mmol) in 10 mL of anhydrous THF at -20° C. was treated with i-butyl chloroformate (0.20 mL, 1.57 mmol) and stirred for 2 min after which a solution of (1R)-4-bromoaminobutane-1-boronic acid (+)-pinanediol ester (522 mg, 1.43 mmol) in 4 mL of anhydrous DMF was added. The reaction mixture was stirred at -20° C. for 15 min, warmed to room temperature over 18 h then poured into EtOAc (ca. 100 mL) and washed with H₂ O (3×25 mL), and saturated aqueous NaCl (1×25 mL), dried (Na₂ SO₄) and concentrated under reduced pressure. The residue was purified by flash chromatography, elution with 3:2 hexanes--EtOAc, to give 306 mg (39%) of the title compound as an oil. LRMS 549, 547 (M+1, base).

Part D. N¹ -[(4R)-2-(2-Phenyl)ethyl-Thiazoline-4-Carboxy]-R-borothioarginine-(+)-pinanediol ester,

A mixture of (1R)-4-bromo-1-[(4R)-2-(2-phenyl)ethyl-thiazoline-4-carbox]amido-1-boronic acid (+)-pinanediol ester (295 mg, 0.54 mmol) and thiourea (82 mg, 1.08 mmol) in 10 mL of EtOH was heated at reflux for 14 h then cooled to room temperature and concentrated under reduced pressure. The residue was purified by size exclusion chromatography on Sephadex LH-20, elution with MeOH, to give a glass which was dissolved in 3 mL of THF and treated with Et₂ O (ca. 10 mL) to give a solid that was washed with Et₂ O (ca. 5 mL) and dried to afford 230 mg (68%) of the title compound. LRMS 543 (M+1, base); HRMS Calcd for C₂₇ H₄₀ BN₄ O₃ S₂ : 543.2635. Found: 543.2643.

The compounds in the following tables were or can be synthesized by the methods discussed previously or by methods familiar to one skilled in the art.

The compounds listed in Tables 1-61 may be prepared using the above examples. It is understood that R¹⁴⁻¹⁶ and R^(A-C) in the tables correspond to independent R13 groups as described within the scope of this application.

                                      TABLE 1                                      __________________________________________________________________________      ##STR96##                                                                                                              Phys                                  Ex X        R.sup.A   R.sup.B                                                                             R.sup.C  Y.sup.l,Y.sup.2                                                                     Data                                  __________________________________________________________________________      1 NHC(NH)NH.sub.2                                                                         H         H    Ph       (+)-pin                                                                             A                                      2 NHC(NH)NH.sub.2                                                                         H         Ph   H        (+)-pin                                                                             BZ                                     3 NHC(NH)NH.sub.2                                                                         H         OPh  Ph       (+)-pin                                                                             B                                      4 NHC(NH)NH.sub.2                                                                         H         H    4-pyridyl                                                                               (+)-pin                                                                             C                                      5 NHC(NH)NH.sub.2                                                                         COPh      H    H        (+)-pin                                     6 NHC(NH)NH.sub.2                                                                         H         COPh H        (+)-pin                                     7 NHC(NH)NH.sub.2                                                                         H         H    COPh     (+)-pin                                     8 NHC(NH)NH.sub.2                                                                         H         NHCbz                                                                               H        (+)-pin                                     9 NHC(NH)NH.sub.2                                                                         H         NMeCbz                                                                              H        (+)-pin                                     10                                                                               NHC(NH)NH.sub.2                                                                         H         H    Et       (+)-pin                                     11                                                                               NHC(NH)NH.sub.2                                                                         H         H    n-Pr     (+)-pin                                     12                                                                               NHC(NH)NH.sub.2                                                                         H         H    i-Pr     (+)-pin                                     13                                                                               NHC(NH)NH.sub.2                                                                         H         H    n-Bu     (+)-pin                                     14                                                                               NHC(NH)NH.sub.2                                                                         H         H    t-Bu     (+)-pin                                     15                                                                               NHC(NH)NH.sub.2                                                                         H         H    n-hexyl  (+)-pin                                     16                                                                               NHC(NH)NH.sub.2                                                                         H         H    cyclohexyl                                                                              (+)-pin                                     17                                                                               NHC(NH)NH.sub.2                                                                         NHCO(CH.sub.2).sub.2 Ph                                                                  H    H        (+)-pin                                     18                                                                               NHC(NH)NH.sub.2                                                                         H         H    O-n-Bu   (+)-pin                                     19                                                                               NHC(NH)NH.sub.2                                                                         H         H    NHCOcyclo-                                                                              (+)-pin                                                               propyl                                               20                                                                               NHC(NH)NH.sub.2                                                                         H         H    NHCO-    (+)-pin                                                               cyclohexyl                                           21                                                                               NHC(NH)NH.sub.2                                                                         H         H    NHCO(4-  (+)-pin                                                               C.sub.6 H.sub.4 OMe)                                 22                                                                               NHC(NH)NH.sub.2                                                                         H         H    4-C.sub.6 H.sub.4 OMe                                                                   (+)-pin                                     23                                                                               NHC(NH)NH.sub.2                                                                         CO.sub.2 CH.sub.2 (2-                                                                    H    H        (+)-pin                                                C.sub.6 H.sub.4 Ph)                                                 24                                                                               NHC(NH)NH.sub.2                                                                         H         H    1-naphthyl                                                                              (+)-pin                                     25                                                                               NHC(NH)NH.sub.2                                                                         H         H    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            (+)-pin                                     26                                                                               NHC(NH)NH.sub.2                                                                         COPh      H    Me       (+)-pin                                     27                                                                               NHC(NH)NH.sub.2                                                                         H         NHCbz                                                                               n-Bu     (+)-pin                                     28                                                                               NHC(NH)NH.sub.2                                                                         H         NMeCbz                                                                              n-Bu     (+)-pin                                     29                                                                               NHC(NH)NH.sub.2                                                                         Me        H    Ph       (+)-pin                                                                             CB                                     30                                                                               NHC(NH)NH.sub.2                                                                         Me        H    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            (+)-pin                                     31                                                                               NHC(NH)NH.sub.2                                                                         H         H    4-C.sub.6 H.sub.4 CO.sub.2 Me                                                           (+)-pin                                     32                                                                               NHC(NH)NH.sub.2                                                                         Me        H    4-C.sub.6 H.sub.4 CO.sub.2 Me                                                           (+)-pin                                     33                                                                               NHC(NH)NH.sub.2                                                                         H         OMe  Ph       (+)-pin                                     34                                                                               SC(NH)NH.sub.2                                                                          H         H    Ph       (+)-pin                                                                             D                                      35                                                                               SC(NH)NH.sub.2                                                                          H         Ph   H        (+)-pin                                                                             E                                      36                                                                               SC(NH)NH.sub.2                                                                          H         OPh  H        (+)-pin                                                                             F                                      37                                                                               SC(NH)NH.sub.2                                                                          COPh      H    H        (+)-pin                                                                             G                                      38                                                                               SC(NH)NH.sub.2                                                                          H         COPh H        (+)-pin                                                                             H                                      39                                                                               SC(NH)NH.sub.2                                                                          H         H    COPh     (+)-pin                                                                             I                                      40                                                                               SC(NH)NH.sub.2                                                                          H         NHCbz                                                                               H        (+)-pin                                                                             J                                      41                                                                               SC(NH)NH.sub.2                                                                          H         NMeCbz                                                                              H        (+)-pin                                                                             K                                      42                                                                               SC(NH)NH.sub.2                                                                          H         H    Et       (+)-pin                                                                             L                                      43                                                                               SC(NH)NH.sub.2                                                                          H         H    n-Pr     (+)-pin                                                                             M                                      44                                                                               SC(NH)NH.sub.2                                                                          H         H    i-Pr     (+)-pin                                                                             N                                      45                                                                               SC(NH)NH.sub.2                                                                          H         H    n-Bu     (+)-pin                                                                             O                                      46                                                                               SC(NH)NH.sub.2                                                                          H         H    t-Eu     (+)-pin                                                                             P                                      47                                                                               SC(NH)NH.sub.2                                                                          H         H    n-hexyl  (+)-pin                                                                             Q                                      48                                                                               SC(NH)NH.sub.2                                                                          H         H    cyclohexyl                                                                              (+)-pin                                                                             R                                      49                                                                               SC(NH)NH.sub.2                                                                          NHCOCH.sub.2 CH.sub.2 Ph                                                                 H    H        (+)-pin                                                                             S                                      50                                                                               SC(NH)NH.sub.2                                                                          H         H    O-n-Bu   (+)-pin                                                                             T                                      51                                                                               SC(NH)NH.sub.2                                                                          H         H    NHCOcyclo-                                                                              (+)-pin                                                                             U                                                                propyl                                               52                                                                               SC(NH)NH.sub.2                                                                          H         H    NHCOcyclo-                                                                              (+)-pin                                                                             V                                                                hexyl                                                53                                                                               SC(NH)NH.sub.2                                                                          H         H    NHCO(4-  (+)-pin                                                                             W                                                                C.sub.6 H.sub.4 OMe)                                 54                                                                               SC(NH)NH.sub.2                                                                          H         H    4-C.sub.6 H.sub.4 OMe                                                                   (+)-pin                                                                             X                                      55                                                                               SC(NH)NH.sub.2                                                                          CO.sub.2 CH.sub.2 (2-                                                                    H    H        (+)-pin                                                                             Y                                                 C.sub.6 H.sub.4 Ph)                                                 56                                                                               SC(NH)NH.sub.2                                                                          H         H    1-naphthyl                                                                              (+)-pin                                     57                                                                               SC(NH)NH.sub.2                                                                          H         H    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            (+)-pin                                     58                                                                               SC(NH)NH.sub.2                                                                          H         NHCbz                                                                               n-Bu     (+)-pin                                                                             Z                                      59                                                                               SC(NH)NH.sub.2                                                                          H         NMeCbz                                                                              n-Bu     (+)-pin                                                                             AA                                     60                                                                               SC(NH)NH.sub.2                                                                          COPh      H    Me       (+)-pin                                                                             BB                                     61                                                                               SC(NH)NH.sub.2                                                                          H         H    4-pyridyl                                                                               (+)-pin                                     62                                                                               SC(NH)NH.sub.2                                                                          Me        H    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            (+)-pin                                     63                                                                               SC(NH)NH.sub.2                                                                          H         H    4-C.sub.6 H.sub.4 CO.sub.2 Me                                                           (+)-pin                                     64                                                                               SC(NH)NH.sub.2                                                                          Me        H    4-C.sub.6 H.sub.4 CO.sub.2 Me                                                           (+)-pin                                     65                                                                               SC(NH)NH.sub.2                                                                          Me        H    Ph       (+)-pin                                     66                                                                               SC(NH)NH.sub.2                                                                          H         OMe  Ph       (+)-pin                                     67                                                                               CH.sub.2 NH.sub.2                                                                       H         H    Ph       (+)-pin                                     68                                                                               CH.sub.2 NH.sub.2                                                                       H         Ph   H        (+)-pin                                                                             YY                                     69                                                                               CH.sub.2 NH.sub.2                                                                       H         OPh  H        (+)-pin                                     70                                                                               CH.sub.2 NH.sub.2                                                                       COPh      H    H        (+)-pin                                     71                                                                               CH.sub.2 NH.sub.2                                                                       H         COPh H        (+)-pin                                     72                                                                               CH.sub.2 NH.sub.2                                                                       H         H    COPh     (+)-pin                                     73                                                                               CH.sub.2 NH.sub.2                                                                       H         NHCbz                                                                               H        (+)-pin                                     74                                                                               CH.sub.2 NH.sub.2                                                                       H         NMeCbz                                                                              H        (+)-pin                                     75                                                                               CH.sub.2 NH.sub.2                                                                       H         H    Et       (+)-pin                                     76                                                                               CH.sub.2 NH.sub.2                                                                       H         H    n-Pr     (+)-pin                                     77                                                                               CH.sub.2 NH.sub.2                                                                       H         H    i-Pr     (+)-pin                                     78                                                                               CH.sub.2 NH.sub.2                                                                       H         H    n-Bu     (+)-pin                                     79                                                                               CH.sub.2 NH.sub.2                                                                       H         H    t-Bu     (+)-pin                                     80                                                                               CH.sub.2 NH.sub.2                                                                       H         H    n-hexyl  (+)-pin                                     81                                                                               CH.sub.2 NH.sub.2                                                                       H         H    cyclohexyl                                                                              (+)-pin                                     82                                                                               CH.sub.2 NH.sub.2                                                                       NHCOCH.sub.2 CH.sub.2 Ph                                                                 H    H        (+)-pin                                     83                                                                               CH.sub.2 NH.sub.2                                                                       H         H    O-n-Bu   (+)-pin                                     84                                                                               CH.sub.2 NH.sub.2                                                                       H         H    NHCOcyclo-                                                                              (+)-pin                                                               propyl                                               85                                                                               CH.sub.2 NH.sub.2                                                                       H         H    NHCOcyclo-                                                                              (+)-pin                                                               hexyl                                                86                                                                               CH.sub.2 NH.sub.2                                                                       H         H    NHCO(4-  (+)-pin                                                               C.sub.6 H.sub.4 OMe)                                 87                                                                               CH.sub.2 NH.sub.2                                                                       H         H    4-C.sub.6 H.sub.4 OMe                                                                   (+)-pin                                     88                                                                               CH.sub.2 NH.sub.2                                                                       CO.sub.2 CH.sub.2 (2-                                                                    H    H        (+)-pin                                                C.sub.6 H.sub.4 Ph)                                                 89                                                                               CH.sub.2 NH.sub.2                                                                       H         H    1-naphthyl                                                                              (+)-pin                                     90                                                                               CH.sub.2 NH.sub.2                                                                       H         H    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            (+)-pin                                     91                                                                               CH.sub.2 NH.sub.2                                                                       H         NHCbz                                                                               n-Bu     (+)-pin                                     92                                                                               CH.sub.2 NH.sub.2                                                                       H         NMeCbz                                                                              n-Bu     (+)-pin                                     93                                                                               CH.sub.2 NH.sub.2                                                                       COPh      H    Me       (+)-pin                                     94                                                                               CH.sub.2 NH.sub.2                                                                       H         H    4-pyridyl                                                                               (+)-pin                                     95                                                                               CH.sub.2 NH.sub.2                                                                       Me        H    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            (+)-pin                                     96                                                                               CH.sub.2 NH.sub.2                                                                       H         H    4-C.sub.6 H.sub.4 CO.sub.2 Me                                                           (+)-pin                                     97                                                                               CH.sub.2 NH.sub.2                                                                       Me        H    4-C.sub.6 H.sub.4 CO.sub.2 Me                                                           (+)-pin                                     98                                                                               CH.sub.2 NH.sub.2                                                                       Me        H    Ph       (+)-pin                                     99                                                                               CH.sub.2 NH.sub.2                                                                       H         OMe  Ph       (+)-pin                                    100                                                                               CH.sub.2 NH.sub.2                                                                       H         OMe  Ph       OH, OH                                     101                                                                               NHC(NH)NH.sub.2                                                                         H         H    Ph       OH, OH                                     102                                                                               NHC(NH)NH.sub.2                                                                         H         Ph   H        OH, OH                                     103                                                                               NHC(NH)NH.sub.2                                                                         H         OPh  Ph       OH, OH                                     104                                                                               NHC(NH)NH.sub.2                                                                         H         H    4-pyridyl                                                                               OH, OH                                     105                                                                               NHC(NH)NH.sub.2                                                                         COPh      H    H        OH, OH                                     106                                                                               NHC(NH)NH.sub.2                                                                         H         COPh H        OH, OH                                     107                                                                               NHC(NH)NH.sub.2                                                                         H         H    COPh     OH, OH                                     108                                                                               NHC(NH)NH.sub.2                                                                         H         NHCbz                                                                               H        OH, OH                                     109                                                                               NHC(NH)NH.sub.2                                                                         H         NMeCbz                                                                              H        OH, OH                                     110                                                                               NHC(NH)NH.sub.2                                                                         H         H    Et       OH, OH                                     111                                                                               NHC(NH)NH.sub.2                                                                         H         H    n-Pr     OH, OH                                     112                                                                               NHC(NH)NH.sub.2                                                                         H         H    i-Pr     OH, OH                                     113                                                                               NHC(NH)NH.sub.2                                                                         H         H    n-Bu     OH, OH                                     114                                                                               NHC(NH)NH.sub.2                                                                         H         H    t-Bu     OH, OH                                     115                                                                               NHC(NH)NH.sub.2                                                                         H         H    n-hexyl  OH, OH                                     116                                                                               NHC(NH)NH.sub.2                                                                         H         H    cyclohexyl                                                                              OH, OH                                     117                                                                               NHC(NH)NH.sub.2                                                                         NHCO(CH.sub.2).sub.2 Ph                                                                  H    H        OH, OH                                     118                                                                               NHC(NH)NH.sub.2                                                                         H         H    O-n-Bu   OH, OH                                     119                                                                               NHC(NH)NH.sub.2                                                                         H         H    NHCOcyclo-                                                                              OH, OH                                                                propyl                                              120                                                                               NHC(NH)NH.sub.2                                                                         H         H    NHCO-    OH, OH                                                                cyclohexyl                                          121                                                                               NHC(NH)NH.sub.2                                                                         H         H    NHCO(4-  OH, OH                                                                C.sub.6 H.sub.4 OMe)                                122                                                                               NHC(NH)NH.sub.2                                                                         H         H    4-C.sub.6 H.sub.4 OMe                                                                   OH, OH                                     123                                                                               NHC(NH)NH.sub.2                                                                         CO.sub.2 CH.sub.2 (2-                                                                    H    H        OH, OH                                                 C.sub.6 H.sub.4 Ph)                                                124                                                                               NHC(NH)NH.sub.2                                                                         H         H    1-naphthyl                                                                              OH, OH                                     125                                                                               NHC(NH)NH.sub.2                                                                         H         H    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OH, OH                                     126                                                                               NHC(NH)NH.sub.2                                                                         COPh      H    Me       OH, OH                                     127                                                                               NHC(NH)NH.sub.2                                                                         H         NHCbz                                                                               n-Bu     OH, OH                                     128                                                                               NHC(NH)NH.sub.2                                                                         H         NMeCbz                                                                              n-Bu     OH, OH                                     129                                                                               NHC(NH)NH.sub.2                                                                         Me        H    Ph       OH, OH                                                                              CD                                    130                                                                               NHC(NH)NH.sub.2                                                                         Me        H    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OH, OH                                     131                                                                               NHC(NH)NH.sub.2                                                                         H         H    4-C.sub.6 H.sub.4 CO.sub.2 Me                                                           OH, OH                                     132                                                                               NHC(NH)NH.sub.2                                                                         Me        H    4-C.sub.6 H.sub.4 CO.sub.2 Me                                                           OH, OH                                     133                                                                               NHC(NH)NH.sub.2                                                                         H         OMe  Ph       OH, OH                                     134                                                                               SC(NH)NH.sub.2                                                                          H         H    Ph       OH, OH                                     135                                                                               SC(NH)NH.sub.2                                                                          H         Ph   H        OH, OH                                     136                                                                               SC(NH)NH.sub.2                                                                          H         OPh  H        OH, OH                                     137                                                                               SC(NH)NH.sub.2                                                                          COPh      H    H        OH, OH                                     138                                                                               SC(NH)NH.sub.2                                                                          H         COPh H        OH, OH                                     139                                                                               SC(NH)NH.sub.2                                                                          H         H    COPh     OH, OH                                     140                                                                               SC(NH)NH.sub.2                                                                          H         NHCbz                                                                               H        OH, OH                                     141                                                                               SC(NH)NH.sub.2                                                                          H         NMeCbz                                                                              H        OH, OH                                     142                                                                               SC(NH)NH.sub.2                                                                          H         H    Et       OH, OH                                     143                                                                               SC(NH)NH.sub.2                                                                          H         H    n-Pr     OH, OH                                     144                                                                               SC(NH)NH.sub.2                                                                          H         H    i-Pr     OH, OH                                     145                                                                               SC(NH)NH.sub.2                                                                          H         H    n-Bu     OH, OH                                     146                                                                               SC(NH)NH.sub.2                                                                          H         H    t-Bu     OH, OH                                     147                                                                               SC(NH)NH.sub.2                                                                          H         H    n-hexyl  OH, OH                                     148                                                                               SC(NH)NH.sub.2                                                                          H         H    cyclohexyl                                                                              OH, OH                                     149                                                                               SC(NH)NH.sub.2                                                                          NHCOCH.sub.2 CH.sub.2 Ph                                                                 H    H        OH, OH                                     150                                                                               SC(NH)NH.sub.2                                                                          H         H    O-n-Bu   OH, OH                                     151                                                                               SC(NH)NH.sub.2                                                                          H         H    NHCOcyclo-                                                                              OH, OH                                                                propyl                                              152                                                                               SC(NH)NH.sub.2                                                                          H         H    NHCOcyclo-                                                                              OH, OH                                                                hexyl                                               153                                                                               SC(NH)NH.sub.2                                                                          H         H    NHCO(4-  OH, OH                                                                C.sub.6 H.sub.4 OMe)                                154                                                                               SC(NH)NH.sub.2                                                                          H         H    4-C.sub.6 H.sub.4 OMe                                                                   OH, OH                                     155                                                                               SC(NH)NH.sub.2                                                                          CO.sub.2 CH.sub.2 (2-                                                                    H    H        OH, OH                                                 C.sub.6 H.sub.4 Ph)                                                156                                                                               SC(NH)NH.sub.2                                                                          H         H    1-naphthyl                                                                              OH, OH                                     157                                                                               SC(NH)NH.sub.2                                                                          H         H    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OH, OH                                     158                                                                               SC(NH)NH.sub.2                                                                          H         NHCbz                                                                               n-Bu     OH, OH                                     159                                                                               SC(NH)NH.sub.2                                                                          H         NMeCbz                                                                              n-Bu     OH, OH                                     160                                                                               SC(NH)NH.sub.2                                                                          COPh      H    Me       OH, OH                                     161                                                                               SC(NH)NH.sub.2                                                                          H         H    4-pyridyl                                                                               OH, OH                                     162                                                                               SC(NH)NH.sub.2                                                                          Me        H    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OH, OH                                     163                                                                               SC(NH)NH.sub.2                                                                          H         H    4-C.sub.6 H.sub.4 CO.sub.2 Me                                                           OH, OH                                     164                                                                               SC(NH)NH.sub.2                                                                          Me        H    4-C.sub.6 H.sub.4 CO.sub.2 Me                                                           OH, OH                                     165                                                                               SC(NH)NH.sub.2                                                                          Me        H    Ph       OH, OH                                     166                                                                               SC(NH)NH.sub.2                                                                          H         OMe  Ph       OH, OH                                     167                                                                               CH.sub.2 NH.sub.2                                                                       H         H    Ph       OH, OH                                     168                                                                               CH.sub.2 NH.sub.2                                                                       H         Ph   H        OH, OH                                     169                                                                               CH.sub.2 NH.sub.2                                                                       H         OPh  H        OH, OH                                     170                                                                               CH.sub.2 NH.sub.2                                                                       COPh      H    H        OH, OH                                     171                                                                               CH.sub.2 NH.sub.2                                                                       H         COPh H        OH, OH                                     172                                                                               CH.sub.2 NH.sub.2                                                                       H         H    COPh     OH, OH                                     173                                                                               CH.sub.2 NH.sub.2                                                                       H         NHCbz                                                                               H        OH, OH                                     174                                                                               CH.sub.2 NH.sub.2                                                                       H         NMeCbz                                                                              H        OH, OH                                     175                                                                               CH.sub.2 NH.sub.2                                                                       H         H    Et       OH, OH                                     176                                                                               CH.sub.2 NH.sub.2                                                                       H         H    n-Pr     OH, OH                                     177                                                                               CH.sub.2 NH.sub.2                                                                       H         H    i-Pr     OH, OH                                     178                                                                               CH.sub.2 NH.sub.2                                                                       H         H    n-Bu     OH, OH                                     179                                                                               CH.sub.2 NH.sub.2                                                                       H         H    t-Bu     OH, OH                                     180                                                                               CH.sub.2 NH.sub.2                                                                       H         H    n-hexyl  OH, OH                                     181                                                                               CH.sub.2 NH.sub.2                                                                       H         H    cyclohexyl                                                                              OH, OH                                     182                                                                               CH.sub.2 NH.sub.2                                                                       NHCOCH.sub.2 CH.sub.2 Ph                                                                 H    H        OH, OH                                     183                                                                               CH.sub.2 NH.sub.2                                                                       H         H    O-n-Bu   OH, OH                                     184                                                                               CH.sub.2 NH.sub.2                                                                       H         H    NHCOcyclo-                                                                              OH, OH                                                                propyl                                              185                                                                               CH.sub.2 NH.sub.2                                                                       H         H    NHCOcyclo-                                                                              OH, OH                                                                hexyl                                               186                                                                               CH.sub.2 NH.sub.2                                                                       H         H    NHCO(4-  OH, OH                                                                C.sub.6 H.sub.4 OMe)                                187                                                                               CH.sub.2 NH.sub.2                                                                       H         H    4-C.sub.6 H.sub.4 OMe                                                                   OH, OH                                     188                                                                               CH.sub.2 NH.sub.2                                                                       CO.sub.2 CH.sub.2 (2-                                                                    H    H        OH, OH                                                 C.sub.6 H.sub.4 Ph)                                                189                                                                               CH.sub.2 NH.sub.2                                                                       H         H    1-naphthyl                                                                              OH, OH                                     190                                                                               CH.sub.2 NH.sub.2                                                                       H         H    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OH, OH                                     191                                                                               CH.sub.2 NH.sub.2                                                                       H         NHCbz                                                                               n-Bu     OH, OH                                     192                                                                               CH.sub.2 NH.sub.2                                                                       H         NMeCbz                                                                              n-Bu     OH, OH                                     193                                                                               CH.sub.2 NH.sub.2                                                                       COPh      H    Me       OH, OH                                     194                                                                               CH.sub.2 NH.sub.2                                                                       H         H    4-pyridyl                                                                               OH, OH                                     195                                                                               CH.sub.2 NH.sub.2                                                                       Me        H    4-C.sub.6 H.sub.4 CO.sub.2 H                                                            OH, OH                                     196                                                                               CH.sub.2 NH.sub.2                                                                       H         H    4-C.sub.6 H.sub.4 CO.sub.2 Me                                                           OH, OH                                     197                                                                               CH.sub.2 NH.sub.2                                                                       Me        H    4-C.sub.6 H.sub.4 CO.sub.2 Me                                                           OH, OH                                     198                                                                               CH.sub.2 NH.sub.2                                                                       Me        H    Ph       OH, OH                                     199                                                                               NH(CNH)NH.sub.2                                                                         F         H    Ph       (+)-pin                                                                             SS                                    200                                                                               NH(CNH)NH.sub.2                                                                         F         H    Ph       OH, OH                                     201                                                                               NH(CNH)NH.sub.2                                                                         NH.sub.2  H    Ph       (+)-pin                                    202                                                                               NH(CNH)NH.sub.2                                                                         NH.sub.2  H    Ph       OH, OH                                     203                                                                               NH(CNH)NH.sub.2                                                                         NO.sub.2  H    Ph       (+)-pin                                                                             TT                                    204                                                                               NH(CNH)NH.sub.2                                                                         NO.sub.2  H    Ph       OH, OH                                     205                                                                               NH(CNH)NH.sub.2                                                                         OH        H    Ph       (+)-pin                                    206                                                                               NH(CNH)NH.sub.2                                                                         OH        H    Ph       OH, OH                                     207                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CF.sub.3                                                                      H    Ph       (+)-pin                                    208                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CF.sub.3                                                                      H    Ph       (+)-pin                                    209                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CH.sub.3                                                                      H    Ph       (+)-pin                                    210                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CH.sub.3                                                                      H    Ph       (+)-pin                                    211                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.2 CN                                                                              H    Ph       (+)-pin                                    212                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.2 CN                                                                              H    Ph       OH, OH                                     213                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.2 CH.sub.2 CN                                                                     H    Ph       (+)-pin                                    214                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.2 CH.sub.2 CN                                                                     H    Ph       OH, OH                                     215                                                                               NH(CNH)NH.sub.2                                                                         OCH.sub.2 CN                                                                             H    Ph       (+)-pin                                    216                                                                               NH(CNH)NH.sub.2                                                                         OCH.sub.2 CN                                                                             H    Ph       OH, OH                                     217                                                                               NH(CNH)NH.sub.2                                                                         SCH.sub.2 CN                                                                             H    Ph       (+)-pin                                    218                                                                               NH(CNH)NH.sub.2                                                                         SCH.sub.2 CN                                                                             H    Ph       OH, OH                                     219                                                                               NH(CNH)NH.sub.2                                                                         NHCH.sub.2 CN                                                                            H    Ph       (+)-pin                                    220                                                                               NH(CNH)NH.sub.2                                                                         NHCH.sub.2 CN                                                                            H    Ph       OH, OH                                     221                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.2 OH                                                                              H    Ph       (+)-pin                                    222                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.2 OH                                                                              H    Ph       OH, OH                                     223                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(t-butyl-                                                                             (+)-pin                                                                             UU                                                               NHSO.sub.2)Ph                                       224                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(t-butyl-                                                                             OH, OH                                                                NHSO.sub.2)Ph                                       225                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(ethyl-                                                                               (+)-pin                                                               NHSO.sub.2)Ph                                       226                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(ethyl-                                                                               OH, OH                                                                NHSO.sub.2)Ph                                       227                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(H.sub.2 NSO.sub.2)                                                                   (+)-pin                                                                             ZZ                                                               Ph                                                  228                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(H.sub.2 NSO.sub.2)                                                                   OH, OH                                                                Ph                                                  229                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(MeCO- (+)-pin                                                               NHSO.sub.2)Ph                                       230                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(MeCO- OH, OH                                                                NHSO.sub.2)Ph                                       231                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(MeOCO-                                                                               (+)-pin                                                                             AB                                                               NHSO.sub.2)Ph                                       232                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(MeOCO-                                                                               OH, OH                                                                NHSO.sub.2)Ph                                       233                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(NH.sub.2)Ph                                                                          (+)-pin                                    234                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(NH.sub.2)Ph                                                                          OH, OH                                     235                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-       (+)-pin                                                               (CH.sub.3 SO.sub.2 NH)                                                         Ph                                                  236                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-       OH, OH                                                                (CH.sub.3 SO.sub.2 NH)                                                         Ph                                                  237                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-       (+)-pin                                                               (CF.sub.3 SO.sub.2 NH)                                                         Ph                                                  238                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-       OH, OH                                                                (CF.sub.3 SO.sub.2 NH)                                                         Ph                                                  239                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(CN.sub.4 H)Ph                                                                        (+)-pin                                    240                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(CN.sub.4 H)Ph                                                                        OH, OH                                     241                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(COOH)Ph                                                                              (+)-pin                                    242                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(COOH)Ph                                                                              OH, OH                                     243                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    3-(NH.sub.2)Ph                                                                          (+)-pin                                    244                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    3-(NH.sub.2)Ph                                                                          OH, OH                                     245                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    3-       (+)-pin                                                               (CH.sub.3 SO.sub.2 NH)                                                         Ph                                                  246                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    3-       OH, OH                                                                (CH.sub.3 SO.sub.2 NH)                                                         Ph                                                  247                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  OH   Ph       (+)-pin                                    248                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  OH   Ph       OH, OH                                     249                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  NH.sub.2                                                                            Ph       (+)-pin                                    250                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  NH.sub.2                                                                            Ph       OH, OH                                     251                                                                               NH(CNH)NH.sub.2                                                                         F         H    2-(t-butyl-                                                                             (+)-pin                                                               NHSO.sub.2)Ph                                       252                                                                               NH(CNH)NH.sub.2                                                                         F         H    2-(t-butyl-                                                                             OH, OH                                                                NHSO.sub.2)Ph                                       253                                                                               NH(CNH)NH.sub.2                                                                         F         H    2-(ethyl-                                                                               (+)-pin                                                               NHSO.sub.2)Ph                                       254                                                                               NH(CNH)NH.sub.2                                                                         F         H    2-(ethyl-                                                                               OH, OH                                                                NHSO.sub.2)Ph                                       255                                                                               NH(CNH)NH.sub.2                                                                         F         H    2-(H.sub.2 NSO.sub.2)                                                                   (+)-pin                                                               Ph                                                  256                                                                               NH(CNH)NH.sub.2                                                                         F         H    2-(H.sub.2 NSO.sub.2)                                                                   OH, OH                                                                Ph                                                  257                                                                               NH (C=NH)NH.sub.2                                                                       F         H    2-(MeCO- (+)-pin                                                               NHSO.sub.2)Ph                                       258                                                                               NH(CNH)NH.sub.2                                                                         F         H    2-(MeCO- OH, OH                                                                NHSO.sub.2)Ph                                       259                                                                               NH(CNH)NH.sub.2                                                                         F         H    2-(MeOCO-                                                                               (+)-pin                                                               NHSO.sub.2)Ph                                       260                                                                               NH(CNH)NH.sub.2                                                                         F         H    2-(MeOCO-                                                                               OH, OH                                                                NHSO.sub.2)Ph                                       261                                                                               NH(CNH)NH.sub.2                                                                         H         H    2-(t-butyl-                                                                             (+)-pin                                                                             AC                                                               NHSO.sub.2)Ph                                       262                                                                               NH(CNH)NH.sub.2                                                                         Cl        H    2-(t-butyl-                                                                             (+)-pin                                                                             CE                                                               NHSO.sub.2)Ph                                       263                                                                               NH(CNH)NH.sub.2                                                                         H         H    2-(t-butyl-                                                                             OH, OH                                                                              AD                                                               NHSO.sub.2)Ph                                       264                                                                               NH(CNH)NH.sub.2                                                                         Cl        H    2-(t-butyl-                                                                             OH, OH                                                                NHSO.sub.2)Ph                                       265                                                                               NH(CNH)NH.sub.2                                                                         Cl        H    2-(ethyl -                                                                              (+)-pin                                                               NHSO.sub.2)Ph                                       266                                                                               NH(CNH)NH.sub.2                                                                         Cl        H    2-(ethyl -                                                                              OH, OH                                                                NHSO.sub.2)Ph                                       267                                                                               NH(CNH)NH.sub.2                                                                         Cl        H    2-(H.sub.2 NSO.sub.2)                                                                   (+)-pin                                                               Ph                                                  268                                                                               NH(CNH)NH.sub.2                                                                         Cl        H    2-(H.sub.2 NSO.sub.2)                                                                   OH, OH                                                                Ph                                                  269                                                                               NH(CNH)NH.sub.2                                                                         Cl        H    2-(MeCO- (+)-pin                                                               NHSO.sub.2)Ph                                       270                                                                               NH(CNH)NH.sub.2                                                                         Cl        H    2-(MeCO- OH, OH                                                                NHSO.sub.2)Ph                                       271                                                                               NH(CNH)NH.sub.2                                                                         Cl        H    2-(MeOCO-                                                                               (+)-pin                                                               NHSO.sub.2)Ph                                       272                                                                               NH(CNH)NH.sub.2                                                                         Cl        H    2-(MeOCO-                                                                               OH, OH                                                                NHSO.sub.2)Ph                                       273                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CH.sub.3                                                                      H    2-(t-butyl-                                                                             (+)-pin                                                               NHSO.sub.2)Ph                                       274                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CH.sub.3                                                                      H    2-(t-butyl-                                                                             OH, OH                                                                NHSO.sub.2)Ph                                       275                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CH.sub.3                                                                      H    2-(ethyl -                                                                              (+)-pin                                                               NHSO.sub.2)Ph                                       276                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CH.sub.3                                                                      H    2-(ethyl-                                                                               OH, OH                                                                NHSO.sub.2)Ph                                       277                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CH.sub.3                                                                      H    2-(H.sub.2 NSO.sub.2)                                                                   (+)-pin                                                               Ph                                                  278                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CH.sub.3                                                                      H    2-(H.sub.2 NSO.sub.2)                                                                   OH, OH                                                                Ph                                                  279                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CH.sub.3                                                                      H    2-(MeCO- (+)-pin                                                               NHSO.sub.2)Ph                                       280                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CH.sub.3                                                                      H    2-(MeCO- OH, OH                                                                NHSO.sub.2)Ph                                       281                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CH.sub.3                                                                      H    2-(MeOCO-                                                                               (+)-pin                                                               NHSO.sub.2)Ph                                       282                                                                               NH(CNH)NH.sub.2                                                                         NHSO.sub.2 CH.sub.3                                                                      H    2-(MeOCO-                                                                               OH, OH                                                                NHSO.sub.2)Ph                                       283                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    3-(t-    (+)-pin                                                                             VV                                                               butylOCO-                                                                      NH)Ph                                               284                                                                               NH (C=NH)NH.sub.2                                                                       CH.sub.3  H    3-(t-    OH, OH                                                                butylOCO-                                                                      NH)Ph                                               285                                                                               NH(CNH)NH.sub.2                                                                         N(Et)2    H    Ph       (+)-pin                                    286                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-((ethyl).sub.2                                                                        (+)-pin                                                                             CF                                    NSO.sub.2)Ph                                                                   287                                                                               NH(CNH)NH.sub.2                                                                         CH.sub.3  H    2-(n-BuOCO-                                                                             (+)-pin                                                               NHSO.sub.2)Ph                                       288                                                                               NH(CNH)NH.sub.2                                                                         NO.sub.2  H    2-(t-butyl-                                                                             (+)-pin                                                                             CG                                                               NHSO.sub.2)Ph                                       289                                                                               NH(CNH)NH.sub.2                                                                         NO.sub.2  H    2-(t-butyl-                                                                             OH, OH                                                                NHSO.sub.2)Ph                                       290                                                                               NH(CNH)NH.sub.2                                                                         NO.sub.2  H    2-(ethyl -                                                                              (+)-pin                                                               NHSO.sub.2)Ph                                       291                                                                               NH(CNH)NH.sub.2                                                                         NO.sub.2  H    2-(ethyl -                                                                              OH, OH                                                                NHSO.sub.2)Ph                                       292                                                                               NH(CNH)NH.sub.2                                                                         NO.sub.2  H    2-(H.sub.2 NSO.sub.2)                                                                   (+)-pin                                                               Ph                                                  293                                                                               NH(CNH)NH.sub.2                                                                         NO.sub.2  H    2-(H.sub.2 NSO.sub.2)                                                                   OH, OH                                                                Ph                                                  294                                                                               NH(CNH)NH.sub.2                                                                         NO.sub.2  H    2 -(MeCO-                                                                               (+)-pin                                                               NHSO.sub.2)Ph                                       295                                                                               NH(CNH)NH.sub.2                                                                         NO.sub.2  H    2-(MeCO- OH, OH                                                                NHSO.sub.2)Ph                                       296                                                                               NH(CNH)NH.sub.2                                                                         NO.sub.2  H    2-(MeOCO-                                                                               (+)-pin                                                               NHSO.sub.2)Ph                                       297                                                                               NH(CNH)NH.sub.2                                                                         NO.sub.2  H    2-(MeOCO-                                                                               OH, OH                                                                NHSO.sub.2)Ph                                       298                                                                               NH(CNH)NH.sub.2                                                                         H         NO.sub.2                                                                            Ph       (+)-pin                                                                             AE                                    299                                                                               NH(CNH)NH.sub.2                                                                         H         NH.sub.2                                                                            Ph       (+)-pin                                                                             AF                                    300                                                                               NH(CNH)NH.sub.2                                                                         H         NO.sub.2                                                                            Ph       OH, OH                                     301                                                                               NH(CNH)NH.sub.2                                                                         H         NH.sub.2                                                                            Ph       OH, OH                                     302                                                                               NH(CNH)H H         H    2-(t-butyl-                                                                             (+)-pin                                                                             CH                                                               NHSO.sub.2)Ph                                       303                                                                               NH(CNH)NH.sub.2                                                                         2-NHBOC   H    Ph       (+)-pin                                                                             CI                                    304                                                                               NH(CNH)NH.sub.2                                                                         2-NO.sub.2                                                                               H    Ph       (+)-pin                                                                             CJ                                    305                                                                               OCH.sub.3                                                                               2-Me      H    2-(H.sub.2 NSO.sub.2)                                                                   (+)-pin                                                                             CK                                                               Ph                                                  306                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-thiophen-                                                                             (+)-pin                                                               2-yl                                                307                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-thiophen-                                                                             (+)-pin                                                               3-yl                                                308                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-thio                                                                              H        (+)-pin                                                          phen-                                                                          2-yl                                                     309                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-thio                                                                              H        (+)-pin                                                          phen-                                                                          3-yl                                                     310                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-furan-2-                                                                              (+)-pin                                                               yl                                                  311                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-furan-3-                                                                              (+)-pin                                                               yl                                                  312                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-   H        (+)-pin                                                          furan-                                                                         2-yl                                                     313                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-   H        (+)-pin                                                          furan-                                                                         3-yl                                                     314                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-imidazol-                                                                             (+)-pin                                                               2-yl                                                315                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-imidazol-                                                                             (+)-pin                                                               4-yl                                                316                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-imid-                                                                             H        (+)-pin                                                          azol-                                                                          2-yl                                                     317                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-imid-                                                                             H        (+)-pin                                                          azol-                                                                          4-yl                                                     318                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-pyrazol-                                                                              (+)-pin                                                               1-yl                                                319                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-pyrazol-2-yl                                                                          (+)-pin                                    320                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-pyra                                                                              H        (+)-pin                                                          zol-1-yl                                                 321                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-pyra                                                                              H        (+)-pin                                                          zol-2-yl                                                 322                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-pyrrol-1-yl                                                                           (+)-pin                                    323                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-pyrrol-2-yl                                                                           (+)-pin                                    324                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-pyrrol-                                                                           H        (+)-pin                                                          1-yl                                                     325                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-pyrrol-                                                                           H        (+)-pin                                                          2-yl                                                     326                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-(1,2,4-                                                                               (+)-pin                                                               triazol-1-yl)                                       327                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-(1,2,4-                                                                               (+)-pin                                                               triazol-2-yl)                                       328                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-(1,2,4-                                                                           H        (+)-pin                                                          triazol-                                                                       1-yl)                                                    329                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-(1,2,4-                                                                           H        (+)-pin                                                          triazol-                                                                       1-yl)                                                    330                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-(1,2,3-                                                                               (+)-pin                                                               triazol-1-                                                                     yl)                                                 331                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-(1,2,3-                                                                               (+)-pin                                                               triazol-4-                                                                     yl)                                                 332                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-   H        (+)-pin                                                          (1,2,3                                                   tri-                                                                                                 azol-                                                                          1-yl)                                                    333                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-   H        (+)-pin                                                          (1,2,3                                                   tri                                                                                                  azol-                                                                          4-yl)                                                    334                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-tetrazol-                                                                             (+)-pin                                                               1-yl                                                335                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-tetrazol-                                                                             (+)-pin                                                               5-yl                                                336                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-   H        (+)-pin                                                          tetra                                                                          zol-1-                                                                         yl                                                       337                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-   H        (+)-pin                                                          tetra                                                                          zol-5-                                                                         yl                                                       338                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-oxazol-2-                                                                             (+)-pin                                                               yl                                                  339                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-oxazol-4-                                                                             (+)-pin                                                               yl                                                  340                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-oxazol-5-                                                                             (+)-pin                                                               yl                                                  341                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-   H        (+)-pin                                                          oxazol                                                   2-yl                                                                           342                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-   H        (+)-pin                                                          oxazol                                                   4-yl                                                                           343                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-   H        (+)-pin                                                          oxazol                                                   5-yl                                                                           344                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-thiazol-                                                                              (+)-pin                                                               2-yl                                                345                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-thiazol-                                                                              (+)-pin                                                               4-yl                                                346                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-thiazol-                                                                              (+)-pin                                                               5-yl                                                347                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-thia                                                                              H        (+)-pin                                                          zol-2-                                                                         yl                                                       348                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-thia                                                                              H        (+)-pin                                                          zol-4-                                                                         yl                                                       349                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-thia                                                                              H        (+)-pin                                                          zol-5-                                                                         yl                                                       350                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-pyridin-                                                                              (+)-pin                                                               2-yl                                                351                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-pyridin-                                                                              (+)-pin                                                               3-yl                                                352                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-pyri                                                                              H        (+)-pin                                                          din-2-                                                                         yl                                                       353                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-pyri                                                                              H        (+)-pin                                                          din-3-                                                                         yl                                                       354                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-pyrimi (+)-pin                                                               din-2-yl                                            355                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-pyrimi (+)-pin                                                               din-4-yl                                            356                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  H    4-pyrimi (+)-pin                                                               din-5-yl                                            357                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-pyri                                                                              H        (+)-pin                                                          midin-                                                                         2-yl                                                     358                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-pyri                                                                              H        (+)-pin                                                          midin-                                                                         4-yl                                                     359                                                                               CH.sub.2 NH.sub.2                                                                       CH.sub.3  3-pyri                                                                              H        (+)-pin                                                          midin-                                                                         S-yl                                                     __________________________________________________________________________      (+)-pin indicates (+)pinanediol                                                A: MS (M+H).sup.+ = 489;                                                       B: MS (DCI - NH.sub.3), 505 (M + H).sup.+.                                     C: MS (M + H).sup.+  = 490.                                                    D: MS (M + H).sup.+  = 506;                                                    E: mp 145-150° C.; MS (DCI - NH.sub.3), Calc: 506, Found: 506.          F: MS (DCI - NH.sub.3), 522 (M + H).sup.+.                                     G: HRMS (DCI - NH.sub.3), Calc: 534.2597, Found: 534.2609.                     H: HRMS (DCI - NH.sub.3), Calc: 534.2597, Found: 534.2605.                     I: HRMS (DCI - NH.sub.3), Calc: 534.2597, Found: 534.2609.                     J: [a].sub.D = -14.85° (c = 0.606, MeOH); MS (CI - NH.sub.3), m/e       (%) 537.2 (10.2, M + H - H.sub.2 NCN).sup.+), 429.0 (42.8), 277.0 (100);       Anal. Calcd for C.sub.30 H.sub.40 BBrN.sub.4 O.sub.5 S: C, 54.64; H, 6.11      N, 8.50; B, 1.64. Found: C, 54.52; H, 6.16; N, 8.45; B, 1.60.                  K: [a].sub.D = -15.07° (c = 0.604, MeOH); MS (CI - NH.sub.3), m/e       (%) 593.2 (1.2, (M + H).sup.+), 568.3 (22, (M + NH.sub.4 - H.sub.2             NCN).sup.+), 551.3 (100, (M + H - H.sub.2 NCN).sup.+); Anal. Calcd for         C.sub.31 H.sub.42 BBrN.sub.4 O.sub.5 S: C, 55.29; H, 6.29; N, 8.32; B,         1.61. Found: C, 55.15; H, 6.21; N, 8.22; B, 1.47.                              L: [a].sub.D = -14.12° (c = 0.602, MeOH); MS (DCI - NH.sub.3), m/e      (%) 458 (100, (M + H).sup.+); Anal. Calcd for C.sub.24 H.sub.37 BBrN.sub.      O.sub.3 S: C, 53.54; H, 6.93; N, 7.81; B, 2.01. Found: C, 53.75; H, 6.98;      N, 7.74; B, 1.97.                                                              M: [a].sub.D = -14.21° (c = 0.556, MeOH); MS (CI - NH.sub.3), m/e       (%) 472.2 (13.5, (M + H).sup.+) , 430.2 (100, (M + H - H.sub.2                 NCN).sup.+), 278.0 (61.9); Anal. Calcd for C.sub.25 H.sub.39 BBrN.sub.3        O.sub.3 S: C, 54.36; H, 7.12; N, 7.61; B, 1.96. Found: C, 54.50; H, 7.18;      N, 7.83; B, 1.73.                                                              N: [a].sub.D = -13.79° (c = 0.602, MeOH); MS (DCI - NH.sub.3), m/e      (%) 472 (100, (M + H).sup.+), 430 (37, (M + H - H.sub.2 NCN).sup.+); Anal      Calcd for C.sub.25 H.sub.39 BBrN.sub.3 O.sub.3 S: C, 54.36; H, 7.12; N,        7.61; B, 1.96. Found: C, 54.64; H, 7.17; N, 7.50; B, 1.74.                     O: [a].sub.D = -13.19° (c = 0.364, MeOH); MS (CI - NH.sub.3), m/e       (%) 486.2 (3.3, (M + H).sup.+), 444.2 (87.1, (M + H - H.sub.2 NCN).sup.+)      292.0 (100); Anal. Calcd for C.sub.26 H.sub.41 BBrN.sub.3 O.sub.3 S: C,        55.13; H, 7.30; N, 7.42; B, 1.91. Found: C, 54.99; H, 7.22; N, 7.29; B,        2.07.                                                                          P: [a].sub.D = -12.71° (c = 0.598, MeOH); MS (DCI - NH.sub.3), m/e      (%) 486 (100, (M + H).sup.+), 444 (16, (M + H - H.sub.2 NCN).sup.+); Anal      Calcd for C.sub.26 H.sub.41 BBrN.sub.3 O.sub.3 S: C, 55.13; H, 7.30; N,        7.42; B, 1.91. Found: C, 55.09; H, 7.45; N, 7.40; B, 1.67.                     Q: MS (DCI - NH.sub.3), m/e (%) 514 (100, (M + H).sup.+), 472 (16, (M + H      - H.sub.2 NCN).sup.+); Anal. Calcd for C.sub.28 H.sub.45 BBrN.sub.3            O.sub.3 S: C, 56.57; H, 7.63; N, 7.07; B, 1.82. Found: C, 56.19; H, 7.53;      N, 6.97; B, 1.99.                                                              R: [a].sub.D = -11.70° (c = 0.530, MeOH); MS (DCI - NH.sub.3), m/e      (%) 512 (100, (M + H).sup.+), 470 (40, (M + H - H.sub.2 NCN).sup.+); Anal      Calcd for C.sub.28 H.sub.43 BBrN.sub.3 O.sub.3 S: C, 56.77; H, 7.32; N,        7.09; B, 1.82. Found: C, 56.49; H, 7.38; N, 6.96; B, 1.75.                     S: HRMS (DCI - NH.sub.3), Calc: 577.3019, Found: 577.3025.                     T: [a].sub.D = -8.31° (c = 0.614, MeOH); MS (DCI - NH.sub.3), m/e       (%) 502 (100, (M + H).sup.+), 460 (28, (M + H - H.sub.2 NCN).sup.+); Anal      Calcd for C.sub.26 H.sub.41 BBrN.sub.3 O.sub.4 S: C, 53.62; H, 7.10; N,        7.21; B, 1.86. Found: C, 53.61; H, 7.09; N, 7.20; B, 1.78.                     U: HRMS (DCI - NH.sub.3), Calc: 513.2707, Found: 513.2702.                     V: HRMS (DCI - NH.sub.3), Calc: 555.3165, Found: 555.3176.                     W: HRMS (DCI - NH.sub.3), Calc: 579.2812, Found: 579.2801.                     X: HRMS (DCI - NH.sub.3), Calc: 450.2962, Found: 450.2958.                     Y: HRMS (DCI - NH.sub.3), Calc: 640.3016, Found: 640.3022.                     Z: [a].sub.D = -8.80° (c = 0.602, MeOH); MS (CI - NH.sub.3), m/e        (%) 593.2 (1.3, (M + H - H.sub.2 NCN).sup.+), 485.2 (42.7), 333.0 (100);       Anal. Calcd for C.sub.34 H.sub.48 BBrN.sub.4 O.sub.5 S: C, 57.07; H, 6.76      N, 7.83; B, 1.51. Found: C, 57.17; H, 6.84; N, 7.76; B, 1.41.                  AA: MS (CI - NH.sub.3), m/e (%) 649.4 (1.9, (M + H).sup.+), 624.4 (31, (M      + NH.sub.4 - H.sub.2 NCN).sup.+), 607.2 (100, (M + H - H.sub.2                 NCN).sup.+), 455.0 (39), 444.0 (29.8); Anal. Calcd for C.sub.35 H.sub.50       BBrN.sub.4 O.sub.5 S: C, 57.62; H, 6.91; N, 7.68; B, 1.48. Found: C,           57.37; H, 6.86; N, 7.64; B, 1.40.                                              BB: HRMS (DCI - NH.sub.3), Calc: 520.2805, Found: 520.2796.                    SS. MS (DCI - NH.sub.3), Calc: 507, Found: 507.                                TT. MS (DCI - NH.sub.3), Calc: 534, Found: 534.                                UU. MS (DCI - NH.sub.3), Calc: 638, Found: 638.                                VV. MS (DCI - NH.sub.3), Calc: 618, Found: 618.                                XX. MS (DCI - NH.sub.3), Calc: 489, Found: 489.                                YY. MS (DCI - NH.sub.3), Calc: 461, Found: 461.                                ZZ. MS (DCI - NH.sub.3), Calc: 582, Found: 582.                                AB. MS (DCI - NH.sub.3), Calc: 641, Found: 641.                                AC. MS (DCI - NH.sub.3), Calc: 625, Found: 625.                                AD. MS (DCI - NH.sub.3), Calc: 490, Found: 490.                                AE. MS (DCI - NH.sub.3), Calc: 534, Found: 534.                                AF. MS (DCI - NH.sub.3), Calc: 504, Found: 504.                                CB. MS (M+H).sup.+, Calc: 503.32, Found: 503.32.                               CD. MS (M+H).sup.+, Calc: , Found: .(WITYAK)                                   CE. MS (M+H).sup.+, Calc: 658, Found: 658.                                     CF. MS (M+H).sup.+, Calc: 638, Found: 638.                                     CG. MS (M+H).sup.+, Calc: 669, Found: 669.                                     CH. MS (M+H).sup.+, Calc: 609, Found: 609.                                     CI. MS (M+H).sup.+, Calc: 604, Found: 604.                                     CJ. MS (M+H).sup.+, Calc: 641, Found: 641.                                     CK. MS (M+H).sup.+, Calc: 555, Found: 555.                               

                  TABLE 2                                                          ______________________________________                                          ##STR97##                                                                     Ex     X           Y        Y.sup.1,Y.sup.2                                                                       Phys Data                                   ______________________________________                                         365    CH.sub.2 NH.sub.2                                                                          CO       (+)-pin                                            366    CH.sub.2 NH.sub.2                                                                          SO.sub.2 (+)-pin                                            367    NHC(NH)NH.sub.2                                                                            CO       (+)-pin                                            368    NHC(NH)NH.sub.2                                                                            SO.sub.2 (+)-pin                                            369    SC(NH)NH.sub.2                                                                             CO       (+)-pin                                                                               CC                                          370    SC(NH)NH.sub.2                                                                             SO.sub.2 (+)-pin                                                                               DD                                          371    CH.sub.2 NH.sub.2                                                                          CO       OH, OH                                             372    CH.sub.2 NH.sub.2                                                                          SO.sub.2 OH, OH                                             373    NHC(NH)NH.sub.2                                                                            CO       OH, OH                                             374    NHC(NH)NH.sub.2                                                                            SO.sub.2 OH, OH                                             375    SC(NH)NH.sub.2                                                                             CO       OH, OH                                             376    SC(NH)NH.sub.2                                                                             SO.sub.2 OH, OH                                             ______________________________________                                          CC: HRMS (DCI - NH.sub.3), Calc: 560.2390, Found: 560.2407.                    DD: HRMS (DCI - NH.sub.3), Calc: 596.2060, Found: 596.2055.              

                  TABLE 3                                                          ______________________________________                                          ##STR98##                                                                     Ex      X            t      Y.sup.1,Y.sup.2                                                                        Phys Data                                  ______________________________________                                         382     NH.sub.2     2      (+)-pin                                            383     SC(NH)NH.sub.2                                                                              2      (+)-pin EE                                         384     SC(NH)NH.sub.2                                                                              1      (+)-pin FF                                         385     NHC(NH)NH.sub.2                                                                             2      (+)-pin                                            386     NHC(NH)NH.sub.2                                                                             1      (+)-pin                                            387     NH.sub.2     2      OH, OH                                             388     SC(NH)NH.sub.2                                                                              2      OH, OH                                             389     SC(NH)NH.sub.2                                                                              1      OH, OH                                             390     NHC(NH)NH.sub.2                                                                             2      OH, OH                                             391     NHC(NH)NH.sub.2                                                                             1      OH, OH                                             ______________________________________                                          EE: HRMS (DCI - NH.sub.3), Calc: 546.2597, Found: 546.2604.                    FF: HRMS (DCI - NH.sub.3), Calc: 534.2597, Found: 534.2609.              

                  TABLE 4                                                          ______________________________________                                          ##STR99##                                                                     Ex       X            Y.sup.1,Y.sup.2                                                                           Phys Data                                     ______________________________________                                         397      CH.sub.2 NH.sub.2                                                                           (+)-pin                                                  398      NHC(NH)NH.sub.2                                                                             (+)-pin                                                  399      SC(NH)NH.sub.2                                                                              (+)-pin    GG                                            400      CH.sub.2 NH.sub.2                                                                           OH, OH                                                   401      NHC(NH)NH.sub.2                                                                             OH, OH                                                   402      SC(NH)NH.sub.2                                                                              OH, OH                                                   ______________________________________                                          GG: HRMS (DCI - NH.sub.3), Calc: 532.2441, Found: 532.2445.              

                  TABLE 5                                                          ______________________________________                                          ##STR100##                                                                    Ex       X            Y.sup.1,Y.sup.2                                                                           Phys Data                                     ______________________________________                                         403      CH.sub.2 NH.sub.2                                                                           (+)-pin                                                  404      NHC(NH)NH.sub.2                                                                             (+)-pin                                                  405      SC(NH)NH.sub.2                                                                              (+)-pin    HH                                            406      CH.sub.2 NH.sub.2                                                                           OH, OH                                                   407      NHC(NH)NH.sub.2                                                                             OH, OH                                                   408      SC(NH)NH.sub.2                                                                              OH, OH                                                   ______________________________________                                          HH: HRMS (DCI - NH.sub.3), Calc: 532.2441, Found: 532.2452.              

                  TABLE 6                                                          ______________________________________                                          ##STR101##                                                                    Ex       X            Y.sup.1,Y.sup.2                                                                           Phys Data                                     ______________________________________                                         436      NHC(NH)NH.sub.2                                                                             (+)-pin                                                  437      SC(NH)NH.sub.2                                                                              (+)-pin    II                                            438      CH.sub.2 NH.sub.2                                                                           (+)-pin                                                  439      NHC(NH)NH.sub.2                                                                             OH, OH                                                   440      SC(NH)NH.sub.2                                                                              OH, OH                                                   441      CH.sub.2 NH.sub.2                                                                           OH, OH                                                   ______________________________________                                          II: HRMS (DCI - NH.sub.3), Calc: 480.2493, Found: 480.2492.              

                  TABLE 7                                                          ______________________________________                                          ##STR102##                                                                    Ex      X            Y      Y.sup.1,Y.sup.2                                                                        Phys Data                                  ______________________________________                                         447     NHC(NH)NH.sub.2                                                                             O      (+)-pin WW                                         448     SC(NH)NH.sub.2                                                                              O      (+)-pin JJ                                         449     CH.sub.2 NH.sub.2                                                                           O      (+)-pin                                            450     NHC(NH)NH.sub.2                                                                             S      (+)-pin                                            451     SC(NH)NH.sub.2                                                                              S      (+)-pin                                            452     CH.sub.2 NH.sub.2                                                                           S      (+)-pin                                            453     NHC(NH)NH.sub.2                                                                             O      OH, OH                                             454     SC(NH)NH.sub.2                                                                              O      OH, OH                                             455     CH.sub.2 NH.sub.2                                                                           O      OH, OH                                             456     NHC(NH)NH.sub.2                                                                             S      OH, OH                                             457     SC(NH)NH.sub.2                                                                              S      OH, OH                                             458     CH.sub.2 NH.sub.2                                                                           S      OH, OH                                             ______________________________________                                          JJ: HRMS (DCI - NH.sub.3), Calc: 496.2441, Found: 496.2449.                    WW. MS (DCI - NH.sub.3), Calc: 345, Found: 345.                          

                  TABLE 8                                                          ______________________________________                                          ##STR103##                                                                    Ex    X           R.sup.B R.sup.C                                                                             Y.sup.1,Y.sup.2                                                                       Phys Data                                ______________________________________                                         464   NHC(NH)NH.sub.2                                                                            H       Ph   (+)-pin                                         465   NHC(NH)NH.sub.2                                                                            OBn     H    (+)-pin                                         466   SC(NH)NH.sub.2                                                                             H       Ph   (+)-pin                                                                               KK                                       467   SC(NH)NH.sub.2                                                                             OBn     H    (+)-pin                                                                               LL                                       468   CH.sub.2 NH.sub.2                                                                          H       Ph   (+)-pin                                                                               CL                                       469   CH.sub.2 NH.sub.2                                                                          OBn     H    (+)-pin                                         470   NHC(NH)NH.sub.2                                                                            H       Ph   OH, OH                                          471   NHC(NH)NH.sub.2                                                                            OBn     H    OH, OH                                          472   SC(NH)NH.sub.2                                                                             H       Ph   OH, OH                                          473   SC(NH)NH.sub.2                                                                             OBn     H    OH, OH                                          474   CH.sub.2 NH.sub.2                                                                          H       Ph   OH, OH CM                                       475   CH.sub.2 NH.sub.2                                                                          OBn     H    OH, OH                                          ______________________________________                                          KK: HRMS (DCI - NH.sub.3), Calc: 507.2601, Found: 507.2592.                    LL: HRMS (DCI - NH.sub.3), Calc: 537.2667, Found: 537.2685.                    CL: Anal. Calc'd. for C.sub.27 H.sub.36 BN.sub.3                               O.sub.3.(HCl).sub.1.7.(H.sub.2 O).sub.2.2 : C, 57.60; H, 7.54; Cl, 10.70;      N, 7.46. Found: C, 57.40; H, 7.23; Cl, 10.78; N, 7.53. MS (M+H).sup.+ :        calc. 462, Found 462.                                                          CM: MS(M+H).sup.+ : Calc: 328, Found: 328.                               

                  TABLE 9                                                          ______________________________________                                          ##STR104##                                                                    Ex       X            Y.sup.1,Y.sup.2                                                                           Phys Data                                     ______________________________________                                         476      NHC(NH)NH.sub.2                                                                             (+)-pin                                                  477      SC(NH)NH.sub.2                                                                              (+)-pin    MM                                            478      CH.sub.2 NH.sub.2                                                                           (+)-pin                                                  479      NHC(NH)NH.sub.2                                                                             OH, OH                                                   480      SC(NH)NH.sub.2                                                                              OH, OH                                                   481      CH.sub.2 NH.sub.2                                                                           OH, OH                                                   ______________________________________                                          MM: HRMS (DCI - NH.sub.3), Calc: 498.2233, Found: 498 2231.              

                  TABLE 10                                                         ______________________________________                                          ##STR105##                                                                    Ex   X           W.sup.1                                                                               W.sup.2                                                                             R.sup.3                                                                             Y.sup.1,Y.sup.2                                                                       Phys Data                             ______________________________________                                         482  NHC(NH)NH.sub.2                                                                            N      CH   H    (+)-pin                                      483  SC(NH)NH.sub.2                                                                             N      CH   H    (+)-pin                                                                               NN                                    484  CH.sub.2 NH.sub.2                                                                          N      CH   H    (+)-pin                                      485  NHC(NH)NH.sub.2                                                                            CH     N    Ph   (+)-pin                                      486  SC(NH)NH.sub.2                                                                             CH     N    Ph   (+)-pin                                                                               OO                                    487  CH.sub.2 NH.sub.2                                                                          CH     N    Ph   (+)-pin                                      488  NHC(NH)NH.sub.2                                                                            N      CH   H    OH, OH                                       489  SC(NH)NH.sub.2                                                                             N      CH   H    OH, OH                                       490  CH.sub.2 NH.sub.2                                                                          N      CH   H    OH, OH                                       491  NHC(NH)NH.sub.2                                                                            CH     N    Ph   OH, OH                                       492  SC(NH)NH.sub.2                                                                             CH     N    Ph   OH, OH                                       493  CH.sub.2 NH.sub.2                                                                          CH     N    Ph   OH, OH                                       ______________________________________                                          NN: HRMS (DCI - NH.sub.3), Calc: 481.2445, Found: 481.2442.                    OO: HRMS (DCI - NH.sub.3), Calc: 557.2758, Found: 557.2754.              

                  TABLE 11                                                         ______________________________________                                          ##STR106##                                                                    Ex       X            Y.sup.1,Y.sup.2                                                                           Phys Data                                     ______________________________________                                         499      NHC(NH)NH.sub.2                                                                             (+)-pin                                                  500      SC(NH)NH.sub.2                                                                              (+)-pin    PP                                            501      CH.sub.2 NH.sub.2                                                                           (+)-pin                                                  502      NHC(NH)NH.sub.2                                                                             OH, OH                                                   503      SC(NH)NH.sub.2                                                                              OH, OH                                                   504      CH.sub.2 NH.sub.2                                                                           OH, OH                                                   ______________________________________                                          PP: HRMS (DCI - NH.sub.3), Calc: 5481.2445, Found: 481.2440.             

                  TABLE 12                                                         ______________________________________                                          ##STR107##                                                                    Ex      X           R.sup.3                                                                               Y.sup.1,Y.sup.2                                                                        Phys Data                                   ______________________________________                                         510     SC(NH)NH.sub.2                                                                             H      (+)-pin QQ                                          ______________________________________                                          QQ: HRNS (NH.sub.3 -CI/DEP), Calc: 503.3193, Found: 503.3199.            

                  TABLE 13                                                         ______________________________________                                          ##STR108##                                                                                                                Phys                               Ex.  m, X        R.sup.A R.sup.B                                                                               R.sup.C                                                                              Y.sup.1,Y.sup.2                                                                      Data                               ______________________________________                                         516  2,          H       NHCO-  H     (+)-  RR                                      SC(NH)NH.sub.2      (CH.sub.2).sub.2 Ph                                                                         pin                                      517  2,          H       Ph     H     (+)-                                          SC(NH)NH.sub.2                   pin                                      518  2,          H       OPh    Ph    (+)-                                          SC(NH)NH.sub.2                   pin                                      519  1,          H       H      4-    (+)-                                          SC(NH)NH.sub.2             pyridyl                                                                              pin                                      520  1,          COPh    H      H     (+)-                                          NHC(NH)NH.sub.2                  pin                                      521  3,          H       COPh   H     (+)-                                          NHC(NH)NH.sub.2                  pin                                      522  3,          H       H      COPh  (+)-                                          NHC(NH)NH.sub.2                  pin                                      ______________________________________                                          RR: HRMS (DCINH.sub.3), Calc: 605.333, Found: 605.3325.                  

                                      TABLE 14                                     __________________________________________________________________________      ##STR109##                                                                    Ex X             m R.sup.13  R.sup.14  Y.sup.1 Y.sup.2                                                                     Phys. Data                         __________________________________________________________________________     528                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        H         (+)-pin                                 529                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        Methyl    (+)-pin                                 530                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        Ethyl     (+)-pin                                 531                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        n-Propyl  (+)-pin                                 532                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        n-Butyl   (+)-pin                                 533                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 534                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 535                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 536                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 537                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 538                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 539                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CN                                                                              (+)-pin                                 540                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 541                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 542                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CF.sub.3  (+)-pin                                 543                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CF.sub.2 CF.sub.3                                                                        (+)-pin                                 544                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 545                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 546                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        F.sub.5 Ph                                                                               (+)-pin                                 547                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 548                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 549                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 550                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 551                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 552                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 553                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 NO.sub.2                                                                        (+)-pin                                 554                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 555                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 556                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 OH                                                                              (+)-pin                                 557                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 558                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 559                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                 560                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 561                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 562                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        Ph        (+)-pin                                 563                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        PhCH.sub.2                                                                               (+)-pin                                                                             AG                                 564                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        Ph(CH.sub.2).sub.2                                                                       (+)-pin                                 565                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        3-NO.sub.2Ph                                                                             (+)-pin                                 566                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        4-NO.sub.2Ph                                                                             (+)-pin                                 567                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        3-CO.sub.2 HPh                                                                           (+)-pin                                 568                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        4-CO.sub.2 HPh                                                                           (+)-pin                                 569                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        3-CN.sub.4 HPh                                                                           (+)-pin                                 570                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        4-CN.sub.4 HPh                                                                           (+)-pin                                 571                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 572                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 573                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        H         (+)-pin                                 574                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        Methyl    (+)-pin                                 575                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        Ethyl     (+)-pin                                 576                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        n-Propyl  (+)-pin                                 577                                                                               NH(CNH)NH.sub.2                                                                              1 Fh        n-Butyl   (+)-pin                                 578                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 579                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 580                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 581                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 582                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 583                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 584                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CN                                                                              (+)-pin                                 585                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 586                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 587                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CF.sub.3  (+)-pin                                 588                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CF.sub.2 CF.sub.3                                                                        (+)-pin                                 589                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 590                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 591                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        F.sub.5Ph (+)-pin                                 592                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 593                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 594                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 595                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 596                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 597                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 598                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 NO.sub.2                                                                        (+)-pin                                 599                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 600                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 601                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 OH                                                                              (+)-pin                                 602                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 603                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 604                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                 605                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 606                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 607                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        Ph        (+)-pin                                 609                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        3-NO.sub.2Ph                                                                             (+)-pin                                 610                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        4-NO.sub.2Ph                                                                             (+)-pin                                 611                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        3-CO.sub.2 HPh                                                                           (+)-pin                                 612                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        4-CO.sub.2 HPh                                                                           (+)-pin                                 613                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        3-CN.sub.4 HPh                                                                           (+)-pin                                 614                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        4-CN.sub.4 HPh                                                                           (+)-pin                                 615                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 616                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 617                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        H         OH, OH                                  618                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        Methyl    OH, OH                                  619                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        Ethyl     OH, OH                                  620                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        n-Propyl  OH, OH                                  621                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        n-Butyl   OH, OH                                  622                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 SCH.sub.3                                                                       OH, OH                                  623                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  624                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  625                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  626                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  627                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  628                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CN                                                                              OH, OH                                  629                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  630                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  631                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CF.sub.3  OH, OH                                  632                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CF.sub.2 CF.sub.3                                                                        OH, OH                                  633                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  634                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  635                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        F.sub.5Ph OH, OH                                  636                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  637                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  638                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  639                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  640                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  641                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  642                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 NO.sub.2                                                                        OH, OH                                  643                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  644                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  645                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 OH                                                                              OH, OH                                  646                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.2 OH                                                                      OH, OH                                  647                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.3 OH                                                                      OH, OH                                  648                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  649                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  650                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  651                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        Ph        OH, OH                                  652                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        PhCH.sub.2                                                                               OH, OH                                                                              AH                                 653                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        Ph(CH.sub.2).sub.2                                                                       OH, OH                                  654                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        3-NO.sub.2Ph                                                                             OH, OH                                  655                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        4-NO.sub.2Ph                                                                             OH, OH                                  656                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        3-CO.sub.2 HPh                                                                           OH, OH                                  657                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        4-CO.sub.2 HPh                                                                           OH, OH                                  658                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        3-CN.sub.4 HPh                                                                           OH, OH                                  659                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        4-CN.sub.4 HPh                                                                           OH, OH                                  660                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        3-(HOCH.sub.2)Ph                                                                         OH, OH                                  661                                                                               CH.sub.2 NH.sub.2                                                                            1 Ph        4-(HOCH.sub.2)Ph                                                                         OH, OH                                  662                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        H         OH, OH                                  663                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        Methyl    OH, OH                                  664                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        Ethyl     OH, OH                                  665                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        n-Propyl  OH, OH                                  666                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        n-Butyl   OH, OH                                  667                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 SCH.sub.3                                                                       OH, OH                                  668                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  669                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  670                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  671                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  672                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  673                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CN                                                                              OH, OH                                  674                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH2CH.sub.2 CN                                                                           OH, OH                                  675                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  676                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CF.sub.3  OH, OH                                  677                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CF.sub.2 CF.sub.3                                                                        OH, OH                                  678                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  679                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  680                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        F.sub.5Ph OH, OH                                  681                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  682                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  683                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  684                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  685                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  686                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  687                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 NO.sub.2                                                                        OH, OH                                  688                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  689                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  690                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 OH                                                                              OH, OH                                  691                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.2 OH                                                                      OH, OH                                  692                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.3 OH                                                                      OH, OH                                  693                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  694                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  695                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  696                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        Ph        OH, OH                                  697                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        PhCH.sub.2                                                                               OH, OH                                  698                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        Ph(CH.sub.2).sub.2                                                                       OH, OH                                  699                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        3-NO.sub.2Ph                                                                             OH, OH                                  700                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        4-NO.sub.2Ph                                                                             OH, OH                                  701                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        3-CO.sub.2 HPh                                                                           OH, OH                                  702                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        4-CO.sub.2 HPh                                                                           OH, OH                                  703                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        3-CN.sub.4 HPh                                                                           OH, OH                                  704                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        4-CN.sub.4 HPh                                                                           OH, OH                                  705                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        3-(HOCH.sub.2)Ph                                                                         OH, OH                                  706                                                                               NH(CNH)NH.sub.2                                                                              1 Ph        4-(HOCH.sub.2)Ph                                                                         OH, OH                                  707                                                                               S(CNH)NH.sub.2                                                                               1 Ph        H         (+)-pin                                 708                                                                               S(CNH)NH.sub.2                                                                               1 Ph        Methyl    (+)-pin                                 709                                                                               S(CNH)NH.sub.2                                                                               1 Ph        Ethyl     (+)-pin                                 710                                                                               S(CNH)NH.sub.2                                                                               1 Ph        n-Propyl  (+)-pin                                 711                                                                               S(CNH)NH.sub.2                                                                               1 Ph        n-Butyl   (+)-pin                                 712                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 713                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 714                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 715                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 716                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 717                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 718                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CN                                                                              (+)-pin                                 719                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 720                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 721                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CF.sub.3  (+)-pin                                 722                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CF.sub.2 CF.sub.3                                                                        (+)-pin                                 723                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 724                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 725                                                                               S(CNH)NH.sub.2                                                                               1 Ph        F.sub.5Ph (+)-pin                                 726                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 727                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 728                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 729                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 730                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 731                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 732                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 NO.sub.2                                                                        (+)-pin                                 733                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 734                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 735                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 OH                                                                              (+)-pin                                 736                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 737                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 738                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                 739                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 740                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 741                                                                               S(CNH)NH.sub.2                                                                               1 Ph        Ph        (+)-pin                                 742                                                                               S(CNH)NH.sub.2                                                                               1 Ph        3-NO.sub.2Ph                                                                             (+)-pin                                 743                                                                               S(CNH)NH.sub.2                                                                               1 Ph        4-NO.sub.2Ph                                                                             (+)-pin                                 744                                                                               S(CNH)NH.sub.2                                                                               1 Ph        3-CO.sub.2 HPh                                                                           (+)-pin                                 745                                                                               S(CNH)NH.sub.2                                                                               1 Ph        4-CO.sub.2 HPh                                                                           (+)-pin                                 746                                                                               S(CNH)NH.sub.2                                                                               1 Ph        3-CN.sub.4 HPh                                                                           (+)-pin                                 747                                                                               S(CNH)NH.sub.2                                                                               1 Ph        4-CN.sub.4 HPh                                                                           (+)-pin                                 748                                                                               S(CNH)NH.sub.2                                                                               1 Ph        3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 749                                                                               S(CNH)NH.sub.2                                                                               1 Ph        4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 750                                                                               S(CNH)NH.sub.2                                                                               1 Ph        H         OH, OH                                  751                                                                               S(CNH)NH.sub.2                                                                               1 Ph        Methyl    OH, OH                                  752                                                                               S(CNH)NH.sub.2                                                                               1 Ph        Ethyl     OH, OH                                  753                                                                               S(CNH)NH.sub.2                                                                               1 Ph        n-Propyl  OH, OH                                  754                                                                               S(CNH)NH.sub.2                                                                               1 Ph        n-Butyl   OH, OH                                  755                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 SCH.sub.3                                                                       OH, OH                                  756                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  757                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  758                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  759                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  760                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  761                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CN                                                                              OH, OH                                  762                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  763                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  764                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CF.sub.3  OH, OH                                  765                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CF.sub.2 CF.sub.3                                                                        OH, OH                                  766                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  767                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  768                                                                               S(CNH)NH.sub.2                                                                               1 Ph        F.sub.5Ph OH, OH                                  769                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  770                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  771                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  772                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  773                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  774                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  775                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 NO.sub.2                                                                        OH, OH                                  776                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  777                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  778                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 OH                                                                              OH, OH                                  779                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.2 OH                                                                      OH, OH                                  780                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.3 OH                                                                      OH, OH                                  781                                                                               S(CNH)NH.sub.2                                                                               1 Ph        CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  782                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  783                                                                               S(CNH)NH.sub.2                                                                               1 Ph        (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  784                                                                               S(CNH)NH.sub.2                                                                               1 Ph        Ph        OH, OH                                  785                                                                               S(CNH)NH.sub.2                                                                               1 Ph        PhCH.sub.2                                                                               OH, OH                                  786                                                                               S(CNH)NH.sub.2                                                                               1 Ph        Ph(CH.sub.2).sub.2                                                                       OH, OH                                  787                                                                               S(CNH)NH.sub.2                                                                               1 Ph        3-NO.sub.2Ph                                                                             OH, OH                                  788                                                                               S(CNH)NH.sub.2                                                                               1 Ph        4-NO.sub.2Ph                                                                             OH, OH                                  789                                                                               S(CNH)NH.sub.2                                                                               1 Ph        3-CO.sub.2 HPh                                                                           OH, OH                                  790                                                                               S(CNH)NH.sub.2                                                                               1 Ph        4-CO.sub.2 HPh                                                                           OH, OH                                  791                                                                               S(CNH)NH.sub.2                                                                               1 Ph        3-CN.sub.4 HPh                                                                           OH, OH                                  792                                                                               S(CNH)NH.sub.2                                                                               1 Ph        4-CN.sub.4 HPh                                                                           OH, OH                                  793                                                                               S(CNH)NH.sub.2                                                                               1 Ph        3-(HOCH.sub.2)Ph                                                                         OH, OH                                  794                                                                               S(CNH)NH.sub.2                                                                               1 Ph        4-(HOCH.sub.2)Ph                                                                         OH, OH                                  795                                                                               CH.sub.2 NH.sub.2                                                                            2 Ph        H         (+)-pin                                 796                                                                               CH.sub.2 NH.sub.2                                                                            2 Ph        H         OH, OH                                  797                                                                               OMe           1 Ph        H         (+)-pin                                 798                                                                               OMe           1 Ph        Methyl    (+)-pin                                 799                                                                               OMe           1 Ph        Ethyl     (+)-pin                                 800                                                                               OMe           1 Ph        n-Propyl  (+)-pin                                 801                                                                               OMe           1 Ph        n-Butyl   (+)-pin                                 802                                                                               OMe           1 Ph        CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 803                                                                               OMe           1 Ph        CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 804                                                                               OMe           1 Ph        CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 805                                                                               OMe           1 Ph        CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 806                                                                               OMe           1 Ph        CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 807                                                                               OMe           1 Ph        CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 808                                                                               OMe           1 Ph        CH.sub.2 CN                                                                              (+)-pin                                 809                                                                               OMe           1 Ph        CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 810                                                                               OMe           1 Ph        CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 811                                                                               OMe           1 Ph        CF.sub.3  (+)-pin                                 812                                                                               OMe           1 Ph        CF.sub.2 CF.sub.3                                                                        (+)-pin                                 813                                                                               OMe           1 Ph        CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 814                                                                               OMe           1 Ph        CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 815                                                                               OMe           1 Ph        F.sub.5Ph (+)-pin                                 816                                                                               OMe           1 Ph        CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 817                                                                               OMe           1 Ph        (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 818                                                                               OMe           1 Ph        (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 819                                                                               OMe           1 Ph        CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 820                                                                               OMe           1 Ph        (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 821                                                                               OMe           1 Ph        (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 822                                                                               OMe           1 Ph        CH.sub.2 NO.sub.2                                                                        (+)-pin                                 823                                                                               OMe           1 Ph        (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 824                                                                               OMe           1 Ph        (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 825                                                                               OMe           1 Ph        CH.sub.2 OH                                                                              (+)-pin                                 826                                                                               OMe           1 Ph        (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 827                                                                               OMe           1 Ph        (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 828                                                                               OMe           1 Ph        CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                 829                                                                               OMe           1 Ph        (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 830                                                                               OMe           1 Ph        (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 831                                                                               OMe           1 Ph        Ph        (+)-pin                                 832                                                                               OMe           1 Ph        PhCH.sub.2                                                                               (+)-pin                                 833                                                                               OMe           1 Ph        Ph(CH.sub.2).sub.2                                                                       (+)-Pin                                 834                                                                               OMe           1 Ph        3-NO.sub.2Ph                                                                             (+)-pin                                 835                                                                               OMe           1 Ph        4-NO.sub.2Ph                                                                             (+)-pin                                 836                                                                               OMe           1 Ph        3-CO.sub.2 HPh                                                                           (+)-pin                                 837                                                                               OMe           1 Ph        4-CO.sub.2 HPh                                                                           (+)-pin                                 838                                                                               OMe           1 Ph        3-CN.sub.4 HPh                                                                           (+)-pin                                 839                                                                               OMe           1 Ph        4-CN.sub.4 HPh                                                                           (+)-pin                                 840                                                                               OMe           1 Ph        3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 841                                                                               OMe           1 Ph        4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 842                                                                               OMe           1 Ph        H         OH, OH                                  843                                                                               OMe           1 Ph        Methyl    OH, OH                                  844                                                                               OMe           1 Ph        Ethyl     OH, OH                                  845                                                                               OMe           1 Ph        n-Propyl  OH, OH                                  846                                                                               OMe           1 Ph        n-Butyl   OH, OH                                  847                                                                               OMe           1 Ph        CH.sub.2 SCH.sub.3                                                                       OH, OH                                  848                                                                               OMe           1 Ph        CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  849                                                                               OMe           1 Ph        CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  850                                                                               OMe           1 Ph        CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  851                                                                               OMe           1 Ph        CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  852                                                                               OMe           1 Ph        CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  853                                                                               OMe           1 Ph        CH.sub.2 CN                                                                              OH, OH                                  854                                                                               OMe           1 Ph        CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  855                                                                               OMe           1 Ph        CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  856                                                                               OMe           1 Ph        CF.sub.3  OH, OH                                  857                                                                               OMe           1 Ph        CF.sub.2 CF.sub.3                                                                        OH, OH                                  858                                                                               OMe           1 Ph        CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  859                                                                               OMe           1 Ph        CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  860                                                                               OMe           1 Ph        F.sub.5Ph OH, OH                                  861                                                                               OMe           1 Ph        CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  862                                                                               OMe           1 Ph        (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  863                                                                               OMe           1 Ph        (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  864                                                                               OMe           1 Ph        CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  865                                                                               OMe           1 Ph        (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  866                                                                               OMe           1 Ph        (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  867                                                                               OMe           1 Ph        CH.sub.2 NO.sub.2                                                                        OH, OH                                  868                                                                               OMe           1 Ph        (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  869                                                                               OMe           1 Ph        (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  870                                                                               OMe           1 Ph        CH.sub.2 OH                                                                              OH, OH                                  871                                                                               OMe           1 Ph        (CH.sub.2).sub.2 OH                                                                      OH, OH                                  872                                                                               OMe           1 Ph        (CH.sub.2).sub.3 OH                                                                      OH, OH                                  873                                                                               OMe           1 Ph        CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  874                                                                               OMe           1 Ph        (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  875                                                                               OMe           1 Ph        (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  876                                                                               OMe           1 Ph        Ph        OH, OH                                  877                                                                               OMe           1 Ph        PhCH.sub.2                                                                               OH, OH                                  878                                                                               OMe           1 Ph        Ph(CH.sub.2).sub.2                                                                       OH, OH                                  879                                                                               OMe           1 Ph        3-NO.sub.2Ph                                                                             OH, OH                                  880                                                                               OMe           1 Ph        4-NO.sub.2Ph                                                                             OH, OH                                  881                                                                               OMe           1 Ph        3-CO.sub.2 HPh                                                                           OH, OH                                  882                                                                               OMe           1 Ph        4-CO.sub.2 HPh                                                                           OH, OH                                  883                                                                               OMe           1 Ph        3-CN.sub.4 HPh                                                                           OH, OH                                  884                                                                               OMe           1 Ph        4-CN.sub.4 HPh                                                                           OH, OH                                  885                                                                               OMe           1 Ph        3-(HOCH.sub.2)Ph                                                                         OH, OH                                  886                                                                               OMe           1 Ph        4-(HOCH.sub.2)Ph                                                                         OH, OH                                  887                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               H         (+)-pin                                                                             AK                                 888                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               Methyl    (+)-pin                                                                             AL                                 889                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               Ethyl     (+)-pin                                 890                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               n-Propyl  (+)-pin                                                                             AM                                 891                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               n-Butyl   (+)-pin                                 892                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 SCH.sub.3                                                                       (+)-pin                                                                             AN                                 893                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 894                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 895                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 896                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 897                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 898                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                                                             CN                                 899                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 900                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CF.sub.3  (+)-pin                                 901                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.3                                                                        (+)-pin                                 902                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 903                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 904                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               F.sub.5Ph (+)-pin                                 905                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                                                             AW                                 906                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 907                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 908                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 909                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 910                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 NO.sub.2                                                                        (+)-pin                                 911                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 912                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 913                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 OH                                                                              (+)-pin                                                                             AO                                 914                                                                               CH.sub.2 NH.sub.2                                                                            2 PhCH.sub.2                                                                               CH.sub.2 OCH.sub.2 Ph                                                                    (+)-pin                                                                             AP                                 915                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 916                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 917                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                                                             CP                                 918                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 919                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 920                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               Ph        (+)-pin                                                                             AQ                                 921                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               PhCH.sub.2                                                                               (+)-pin                                                                             AR                                 922                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               Ph(CH.sub.2).sub.2                                                                       (+)-pin                                 923                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-NO.sub.2Ph                                                                             (+)-pin                                                                             AS                                 924                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-NO.sub.2Ph                                                                             (+)-pin                                 925                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CO.sub.2 HPh                                                                           (+)-pin                                 926                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-CO.sub.2 HPh                                                                           (+)-pin                                 927                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CN.sub.4 HPh                                                                           (+)-pin                                 928                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-CN.sub.4 HPh                                                                           (+)-pin                                 929                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 930                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 931                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-NH.sub.2Ph                                                                             (+)-pin                                                                             CQ                                 932                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               H         (+)-pin                                 933                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               Methyl    (+)-pin                                 934                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               Ethyl     (+)-pin                                 935                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               n-Propyl  (+)-pin                                 936                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               n-Butyl   (+)-pin                                 937                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 938                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 939                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 940                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 941                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 942                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 943                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 944                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 945                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 946                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CF.sub.3  (+)-pin                                 947                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.3                                                                        (+)-pin                                 948                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 949                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 950                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               F.sub.5Ph (+)-pin                                 951                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 952                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 953                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 954                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 955                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 956                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 957                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 NO.sub.2                                                                        (+)-pin                                 958                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 959                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 960                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 OH                                                                              (+)-pin                                 961                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 962                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 963                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                 964                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 965                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 966                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               Ph        (+)-pin                                 967                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               PhCH.sub.2                                                                               (+)-pin                                                                             AT                                 968                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               Ph(CH.sub.2).sub.2                                                                       (+)-pin                                 969                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               3-NO.sub.2Ph                                                                             (+)-pin                                                                             AU                                 970                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               4-NO.sub.2Ph                                                                             (+)-pin                                 971                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               3-CO.sub.2 HPh                                                                           (+)-pin                                 972                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               4-CO.sub.2 HPh                                                                           (+)-pin                                 973                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               3-CN.sub.4 HPh                                                                           (+)-pin                                 974                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               4-CN.sub.4 HPh                                                                           (+)-pin                                 975                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 976                                                                               NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 977                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               H         OH, OH                                                                              AI                                 978                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               Methyl    OH, OH                                  979                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               Ethyl     OH, OH                                  980                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               n-Propyl  OH, OH                                  981                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               n-Butyl   OH, OH                                  982                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 SCH.sub.3                                                                       OH, OH                                  983                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  984                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  985                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  986                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  987                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  988                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  989                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  990                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  991                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CF.sub.3  OH, OH                                  992                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.3                                                                        OH, OH                                  993                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  994                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  995                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               F.sub.5Ph OH, OH                                  996                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  987                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  998                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  999                                                                               CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  1000                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  1001                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  1002                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 NO.sub.2                                                                        OH, OH                                  1003                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  1004                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  1005                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 OH                                                                              OH, OH                                  1006                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 OH                                                                      OH, OH                                  1007                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 OH                                                                      OH, OH                                  1008                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  1009                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  1010                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  1011                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               Ph        OH, OH                                                                              AV                                 1012                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               PhCH.sub.2                                                                               OH, OH                                  1013                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               Ph(CH.sub.2).sub.2                                                                       OH, OH                                  1014                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-NO.sub.2Ph                                                                             OH, OH                                  1015                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-NO.sub.2Ph                                                                             OH, OH                                  1016                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CO.sub.2 HPh                                                                           OH, OH                                  1017                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-CO.sub.2 HPh                                                                           OH, OH                                  1018                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CN.sub.4 HPh                                                                           OH, OH                                  1019                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-CN.sub.4 HPh                                                                           OH, OH                                  1020                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-(HOCH.sub.2)Ph                                                                         OH, OH                                  1021                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-(HOCH.sub.2)Ph                                                                         OH, OH                                  1022                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               F         (+)-pin                                 1023                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               Cl        (+)-pin                                 1024                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               Br        (+)-pin                                 1025                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               I         (+)-pin                                 1026                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               COOH      (+)-pin                                 1027                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               COOMe     (+)-pin                                 1028                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CHO       (+)-pin                                 1029                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               COMe      (+)-pin                                 1030                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               NO.sub.2  (+)-pin                                 1031                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CN        (+)-pin                                 1032                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               isopropyl (+)-pin                                 1033                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-F-phenyl                                                                               (+)-pin                                 1034                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-Cl-phenyl                                                                              (+)-pin                                 1035                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-Br-phenyl                                                                              (+)-pin                                 1036                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-I-phenyl                                                                               (+)-pin                                 1037                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CH.sub.3 -phenyl                                                                       (+)-pin                                 1038                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-MeO-phenyl                                                                             (+)-pin                                 1039                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CN-phenyl                                                                              (+)-pin                                 1040                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-CN-phenyl                                                                              (+)-pin                                 1041                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-NC-phenyl                                                                              (+)-pin                                 1042                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-NC-phenyl                                                                              (+)-pin                                 1043                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CF.sub.3 -phenyl                                                                       (+)-pin                                 1044                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CH.sub.3 S-phenyl                                                                      (+)-pin                                 1045                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CH.sub.3 SO-phenyl                                                                     (+)-pin                                 1046                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CH.sub.3 SO.sub.2 -phenyl                                                              (+)-pin                                 1047                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-N(Me).sub.2 -phenyl                                                                    (+)-pin                                 1048                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-MeCO-phenyl                                                                            (+)-pin                                 1049                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CHO-phenyl                                                                             (+)-pin                                 1050                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CO.sub.2 Me-phenyl                                                                     (+)-pin                                 1051                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CONH.sub.2 -phenyl                                                                     (+)-pin                                 1052                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 NHSO.sub.2 CF.sub.3                                                             (+)-pin                                 1053                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 NHSO.sub.2 CH.sub.3                                                             (+)-pin                                 1054                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 -i-propyl                                                              (+)-pin                                 1055                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CHO                                                                             (+)-pin                                 1056                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 OMe                                                                    (+)-pin                                 1057                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 O-i-propyl                                                             (+)-pin                                 1058                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 OCOMe                                                                           (+)-pin                                 1059                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 OCO-i-propyl                                                                    (+)-pin                                 1060                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 OCO-Phenyl                                                                      (+)-pin                                 1061                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 NHCOMe                                                                          (+)-pin                                 1062                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 NHCO-i-propyl                                                                   (+)-pin                                 1063                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               F         OH, OH                                  1064                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               Cl        OH, OH                                  1065                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               Br        OH, OH                                  1066                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               I         OH, OH                                  1067                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               COOH      OH, OH                                  1068                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               COOMe     OH, OH                                  1069                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CHO       OH, OH                                  1070                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               COMe      OH, OH                                  1071                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               NO.sub.2  OH, OH                                  1072                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CN        OH, OH                                  1073                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               isopropyl OH, OH                                  1074                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-F-phenyl                                                                               OH, OH                                  1075                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-Cl-phenyl                                                                              OH, OH                                  1076                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-Br-phenyl                                                                              OH, OH                                  1077                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-I-phenyl                                                                               OH, OH                                  1078                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CH.sub.3 -phenyl                                                                       OH, OH                                  1079                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-MeO-phenyl                                                                             OH, OH                                  1080                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CN-phenyl                                                                              OH, OH                                  1081                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-CN-phenyl                                                                              OH, OH                                  1082                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-NC-phenyl                                                                              OH, OH                                  1083                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               4-NC-phenyl                                                                              OH, OH                                  1084                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CF.sub.3 -phenyl                                                                       OH, OH                                  1085                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CH.sub.3 S-phenyl                                                                      OH, OH                                  1086                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CH.sub.3 SO-phenyl                                                                     OH, OH                                  1087                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CH.sub.3 SO.sub.2 -phenyl                                                              OH, OH                                  1088                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-N(Me).sub.2 -phenyl                                                                    OH, OH                                  1089                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-MeCO-phenyl                                                                            OH, OH                                  1090                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CHO-phenyl                                                                             OH, OH                                  1091                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CO.sub.2 Me-phenyl                                                                     OH, OH                                  1092                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-CONH.sub.2 -phenyl                                                                     OH, OH                                  1093                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 NHSO.sub.2 CF.sub.3                                                             OH, OH                                  1094                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 NHSO.sub.2 CH.sub.3                                                             OH, OH                                  1095                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 -i-propyl                                                              OH, OH                                  1096                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CHO                                                                             OH, OH                                  1097                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 OMe                                                                    OH, OH                                  1098                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 O-i-propyl                                                             OH, OH                                  1099                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 OCOMe                                                                           OH, OH                                  1100                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 OCO-i-propyl                                                                    OH, OH                                  1101                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 OCO-Phenyl                                                                      OH, OH                                  1102                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 NHCOMe                                                                          OH, OH                                  1103                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 NHCO-i-propy1                                                                   OH, OH                                  1104                                                                              CH.sub.2 NH.sub.2                                                                            1 3,4-Di-FPhCH.sub.2                                                                       CH.sub.2 CN                                                                              (+)-pin                                 1105                                                                              CH.sub.2 NH.sub.2                                                                            1 3,4-Di-ClPhCH.sub.2                                                                      CH.sub.2 CN                                                                              (+)-pin                                 1106                                                                              CH.sub.2 NH.sub.2                                                                            1 4-BrPhCH.sub.2                                                                           CH.sub.2 CN                                                                              (+)-pin                                 1107                                                                              CH.sub.2 NH.sub.2                                                                            1 4-IPhCH.sub.2                                                                            CH.sub.2 CN                                                                              (+)-pin                                 1108                                                                              CH.sub.2 NH.sub.2                                                                            1 4-MePhCH.sub.2                                                                           CH.sub.2 CN                                                                              (+)-pin                                 1109                                                                              CH.sub.2 NH.sub.2                                                                            1 2-MeOPhCH.sub.2                                                                          CH.sub.2 CN                                                                              (+)-pin                                 1110                                                                              CH.sub.2 NH.sub.2                                                                            1 2-CNPhCH.sub.2                                                                           CH.sub.2 CN                                                                              (+)-pin                                 1111                                                                              CH.sub.2 NH.sub.2                                                                            1 2-NCPhCH.sub.2                                                                           CH.sub.2 CN                                                                              (+)-pin                                 1112                                                                              CH.sub.2 NH.sub.2                                                                            1 2-NO.sub.2PhCH.sub.2                                                                     CH.sub.2 CN                                                                              (+)-pin                                 1113                                                                              CH.sub.2 NH.sub.2                                                                            1 2-CF.sub.3PhCH.sub.2                                                                     CH.sub.2 CN                                                                              (+)-pin                                 1114                                                                              CH.sub.2 NH.sub.2                                                                            1 2-MeSPhCH.sub.2                                                                          CH.sub.2 CN                                                                              (+)-pin                                 1115                                                                              CH.sub.2 NH.sub.2                                                                            1 3-MeSOPhCH.sub.2                                                                         CH.sub.2 CN                                                                              (+)-pin                                 1116                                                                              CH.sub.2 NH.sub.2                                                                            1 3-MeSO.sub.2PhCH.sub.2                                                                   CH.sub.2 CN                                                                              (+)-pin                                 1117                                                                              CH.sub.2 NH.sub.2                                                                            1 2-NH.sub.2PhCH.sub.2                                                                     CH.sub.2 CN                                                                              (+)-pin                                 1118                                                                              CH.sub.2 NH.sub.2                                                                            1 3-NHMePhCH.sub.2                                                                         CH.sub.2 CN                                                                              (+)-pin                                 1119                                                                              CH.sub.2 NH.sub.2                                                                            1 2-CHOPhCH.sub.2                                                                          CH.sub.2 CN                                                                              (+)-pin                                 1120                                                                              CH.sub.2 NH.sub.2                                                                            1 3-MeCOPhCH.sub.2                                                                         CH.sub.2 CN                                                                              (+)-pin                                 1121                                                                              CH.sub.2 NH.sub.2                                                                            1 2-MeO.sub.2 CPhCH.sub.2                                                                  CH.sub.2 CN                                                                              (+)-pin                                 1122                                                                              CH.sub.2 NH.sub.2                                                                            1 2-NH.sub.2 OCPhCH.sub.2                                                                  CH.sub.2 CN                                                                              (+)-pin                                 1123                                                                              CH.sub.2 NH.sub.2                                                                            1 2-HOCH.sub.2PhCH.sub.2                                                                   CH.sub.2 CN                                                                              (+)-pin                                 1124                                                                              CH.sub.2 NH.sub.2                                                                            1 3,4-Di-FPhCH.sub.2                                                                       CH.sub.2 CN                                                                              OH, OH                                  1125                                                                              CH.sub.2 NH.sub.2                                                                            1 3,4-Di-ClPhCH.sub.2                                                                      CH.sub.2 CN                                                                              OH, OH                                  1126                                                                              CH.sub.2 NH.sub.2                                                                            1 4-BrPhCH.sub.2                                                                           CH.sub.2 CN                                                                              OH, OH                                  1127                                                                              CH.sub.2 NH.sub.2                                                                            1 4-IPhCH.sub.2                                                                            CH.sub.2 CN                                                                              OH, OH                                  1128                                                                              CH.sub.2 NH.sub.2                                                                            1 4-MePhCH.sub.2                                                                           CH.sub.2 CN                                                                              OH, OH                                  1129                                                                              CH.sub.2 NH.sub.2                                                                            1 2-MeOPhCH.sub.2                                                                          CH.sub.2 CN                                                                              OH, OH                                  1130                                                                              CH.sub.2 NH.sub.2                                                                            1 2-CNPhCH.sub.2                                                                           CH.sub.2 CN                                                                              OH, OH                                  1131                                                                              CH.sub.2 NH.sub.2                                                                            1 2-NCPhCH.sub.2                                                                           CH.sub.2 CN                                                                              OH, OH                                  1132                                                                              CH.sub.2 NH.sub.2                                                                            1 2-NO.sub.2PhCH.sub.2                                                                     CH.sub.2 CN                                                                              OH, OH                                  1133                                                                              CH.sub.2 NH.sub.2                                                                            1 2-CF.sub.3PhCH.sub.2                                                                     CH.sub.2 CN                                                                              OH, OH                                  1134                                                                              CH.sub.2 NH.sub.2                                                                            1 2-MeSPhCH.sub.2                                                                          CH.sub.2 CN                                                                              OH, OH                                  1135                                                                              CH.sub.2 NH.sub.2                                                                            1 3-MeSOPhCH.sub.2                                                                         CH.sub.2 CN                                                                              OH, OH                                  1136                                                                              CH.sub.2 NH.sub.2                                                                            1 3-MeSO.sub.2PhCH.sub.2                                                                   CH.sub.2 CN                                                                              OH, OH                                  1137                                                                              CH.sub.2 NH.sub.2                                                                            1 2-NH.sub.2PhCH.sub.2                                                                     CH.sub.2 CN                                                                              OH, OH                                  1138                                                                              CH.sub.2 NH.sub.2                                                                            1 3-NHMePhCH.sub.2                                                                         CH.sub.2 CN                                                                              OH, OH                                  1139                                                                              CH.sub.2 NH.sub.2                                                                            1 2-CHOPhCH.sub.2                                                                          CH.sub.2 CN                                                                              OH, OH                                  1140                                                                              CH.sub.2 NH.sub.2                                                                            1 3-MeCOPhCH.sub.2                                                                         CH.sub.2 CN                                                                              OH, OH                                  1141                                                                              CH.sub.2 NH.sub.2                                                                            1 2-MeO.sub.2 CPhCH.sub.2                                                                  CH.sub.2 CN                                                                              OH, OH                                  1142                                                                              CH.sub.2 NH.sub.2                                                                            1 2-NH.sub.2 OCPhCH.sub.2                                                                  CH.sub.2 CN                                                                              OH, OH                                  1143                                                                              CH.sub.2 NH.sub.2                                                                            1 2-HOCH.sub.2PhCH.sub.2                                                                   CH.sub.2 CN                                                                              OH, OH                                  1144                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               H         OH, OH                                  1145                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               Methyl    OH, OH                                  1146                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               Ethyl     OH, OH                                  1147                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               n-Propyl  OH, OH                                  1148                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               n-Butyl   OH, OH                                  1149                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 SCH.sub.3                                                                       OH, OH                                  1150                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  1151                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  1152                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  1153                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  1154                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  1155                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1156                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  1157                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  1158                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CF.sub.3  OH, OH                                  1159                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.3                                                                        OH, OH                                  1160                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  1161                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  1162                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               F.sub.5PH OH, OH                                  1163                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  1164                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  1165                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  1166                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  1167                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  1168                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  1169                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 NO.sub.2                                                                        OH, OH                                  1170                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  1171                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  1172                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 OH                                                                              OH, OH                                  1173                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 OH                                                                      OH, OH                                  1174                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 OH                                                                      OH, OH                                  1175                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  1176                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  1177                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  1178                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               Ph        OH, OH                                  1179                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               PhCH.sub.2                                                                               OH, OH                                  1180                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               Ph(CH.sub.2).sub.2                                                                       OH, OH                                  1181                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               3-NO.sub.2Ph                                                                             OH, OH                                  1182                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               4-NO.sub.2Ph                                                                             OH, OH                                  1183                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               3-CO.sub.2 HPh                                                                           OH, OH                                  1184                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               4-CO.sub.2 HPh                                                                           OH, OH                                  1185                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               3-CN.sub.4 HPh                                                                           OH, OH                                  1186                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               4-CN.sub.4 HPh                                                                           OH, OH                                  1187                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               3-(HOCH.sub.2)Ph                                                                         OH, OH                                  1188                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               4-(HOCH.sub.2)Ph                                                                         OH, OH                                  1189                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CHO                                                                             (+)-pin                                 1190                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CHO                                                                             OH, OH                                  1191                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CHO                                                                             (+)-pin                                 1192                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CHO                                                                             OH, OH                                  1193                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               H         (+)-pin                                 1194                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               Methyl    (+)-pin                                 1195                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               Ethyl     (+)-pin                                 1196                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               n-Propyl  (+)-pin                                 1197                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               n-Butyl   (+)-pin                                 1198                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 1199                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 1200                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 1201                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 1202                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 1203                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 1204                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1205                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 1206                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 1207                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CF.sub.3  (+)-pin                                 1208                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.3                                                                        (+)-pin                                 1209                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 1210                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 1211                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               F.sub.5Ph (+)-pin                                 1212                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 1213                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 1214                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 1215                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 1216                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 1217                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 1218                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 NO.sub.2                                                                        (+)-pin                                 1219                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 1220                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 1221                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 OH                                                                              (+)-pin                                 1222                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 1223                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 1224                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                 1225                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 1226                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 1227                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               Ph        (+)-pin                                 1228                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               PhCH.sub.2                                                                               (+)-pin                                 1229                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               Ph(CH.sub.2).sub.2                                                                       (+)-pin                                 1230                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               3-NO.sub.2Ph                                                                             (+)-pin                                 1231                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               4-NO.sub.2Ph                                                                             (+)-pin                                 1232                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               3-CO.sub.2 HPh                                                                           (+)-pin                                 1233                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               4-CO.sub.2 HPh                                                                           (+)-pin                                 1234                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               3-CN.sub.4 HPh                                                                           (+)-pin                                 1235                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               4-CN.sub.4 HPh                                                                           (+)-pin                                 1236                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1237                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1238                                                                              CN            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1239                                                                              NO.sub.2      1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1240                                                                              CH.sub.2 NO.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1241                                                                              CF.sub.3      1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1242                                                                              NH.sub.2      1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1243                                                                              NHOH          1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1244                                                                              NHOMe         1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1245                                                                              CH.sub.2 NHOH 1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1246                                                                              CH.sub.2 NHOMe                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1247                                                                              NH(CNH)CH.sub.3                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1248                                                                              NH(CNH)NHOH   1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1249                                                                              NH(CNH)NHNH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1250                                                                              NH(CNH)NHCN   1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1251                                                                              NH(CNH)NHCH.sub.3                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1252                                                                              NH(CNH)NHCOCH.sub.3                                                                          1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1253                                                                              C(NH)NH.sub.2 1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1254                                                                              C(NH)NHMe     1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1255                                                                              C(NH)NHCOMe   1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1256                                                                              --CONH.sub.2  1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1257                                                                              CONHCH.sub.3  1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1258                                                                              CO.sub.2 CH.sub.3                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1259                                                                              OH            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1260                                                                              CH.sub.2 OH   1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1261                                                                              SCH.sub.3     1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1262                                                                              SOCH.sub.3    1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1263                                                                              SO.sub.2 CH.sub.3                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1264                                                                              S(CNH)NHCH.sub.3                                                                             1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1265                                                                              S(CNH)NHCOCH.sub.3                                                                           1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1266                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               H         OH, OH                                  1267                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               Methyl    OH, OH                                  1268                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               Ethyl     OH, OH                                  1269                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               n-Propyl  OH, OH                                  1270                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               n-Butyl   OH, OH                                  1271                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 SCH.sub.3                                                                       OH, OH                                  1272                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  1273                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  1274                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  1275                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  1276                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  1277                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1278                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  1279                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  1280                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CF.sub.3  OH, OH                                  1281                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.3                                                                        OH, OH                                  1282                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  1283                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  1284                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               F.sub.5Ph OH, OH                                  1285                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  1286                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  1287                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  1288                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  1289                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  1290                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  1291                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 NO.sub.2                                                                        OH, OH                                  1292                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  1293                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  1294                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 OH                                                                              OH, OH                                  1295                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 OH                                                                      OH, OH                                  1296                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 OH                                                                      OH, OH                                  1297                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  1298                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  1299                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  1300                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               Ph        OH, OH                                  1301                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               PhCH.sub.2                                                                               OH, OH                                  1302                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               Ph(CH.sub.2).sub.2                                                                       OH, OH                                  1303                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               3-NO.sub.2Ph                                                                             OH, OH                                  1304                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               4-NO.sub.2Ph                                                                             OH, OH                                  1305                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               3-CO.sub.2 HPh                                                                           OH, OH                                  1306                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               4-CO.sub.2 HPh                                                                           OH, OH                                  1307                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               3-CN.sub.4 HPh                                                                           OH, OH                                  1308                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               4-CN.sub.4 HPh                                                                           OH, OH                                  1309                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               3-(HOCH.sub.2)Ph                                                                         OH, OH                                  1310                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2                                                                               4-(HOCH.sub.2)Ph                                                                         OH, OH                                  1311                                                                              CN            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1312                                                                              NO.sub.2      1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1313                                                                              CH.sub.2 NO.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1314                                                                              CF.sub.3      1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1315                                                                              NH.sub.2      1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1316                                                                              NHOH          1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1317                                                                              NHMe          1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1318                                                                              CH.sub.2 NHOH 1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1319                                                                              CH.sub.2 NHOMe                                                                               1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1320                                                                              NH(CNH)CH.sub.3                                                                              1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1321                                                                              NH(CNH)NHOH   1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1322                                                                              NH(CNH)NHNH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1323                                                                              NH(CNH)NHCN   1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1324                                                                              NH(CNH)NHCH.sub.3                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1325                                                                              NH(CNH)NHCOCH.sub.3                                                                          1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1326                                                                              C(NH)NH.sub.2 1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1327                                                                              C(NH)NHMe     1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1328                                                                              C(NH)NHCOMe   1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1329                                                                              CONH.sub.2    1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1330                                                                              CONHCH.sub.3  1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1331                                                                              CO.sub.2 CH.sub.3                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1332                                                                              OH            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1333                                                                              CH.sub.2 OH   1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1334                                                                              SCH.sub.3     1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1335                                                                              SOCH.sub.3    1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1336                                                                              SO.sub.2 CH.sub.3                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1337                                                                              S(CNH)NHCH.sub.3                                                                             1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1338                                                                              S(CNH)NHCOCH.sub.3                                                                           1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1339                                                                              CH.sub.2 NH.sub.2                                                                            2 PhCH.sub.2                                                                               H         (+)-pin                                 1340                                                                              CH.sub.2 NH.sub.2                                                                            2 PhCH.sub.2                                                                               H         OH, OH                                  1341                                                                              OMe           1 PhCH.sub.2                                                                               H         (+)-pin                                 1342                                                                              OMe           1 PhCH.sub.2                                                                               Methyl    (+)-pin                                 1343                                                                              OMe           1 PhCH.sub.2                                                                               Ethyl     (+)-pin                                 1344                                                                              OMe           1 PhCH.sub.2                                                                               n-Propyl  (+)-pin                                 1345                                                                              OMe           1 PhCH.sub.2                                                                               n-Butyl   (+)-pin                                 1346                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 1347                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 1348                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 1349                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 1350                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 1351                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 1352                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-Pin                                                                             CR                                 1353                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 1354                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 1355                                                                              OMe           1 PhCH.sub.2                                                                               CF.sub.3  (+)-pin                                 1356                                                                              OMe           1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.3                                                                        (+)-pin                                 1357                                                                              OMe           1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 1358                                                                              OMe           1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 1359                                                                              OMe           1 PhCH.sub.2                                                                               F.sub.5Ph (+)-pin                                 1360                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 1361                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 1362                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 1363                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 1364                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 1365                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 1366                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 NO.sub.2                                                                        (+)-pin                                 1367                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 1368                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 1369                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 OH                                                                              (+)-pin                                 1370                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 1371                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 1372                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                 1373                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 1374                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 1375                                                                              OMe           1 PhCH.sub.2                                                                               Ph        (+)-pin                                 1376                                                                              OMe           1 PhCH.sub.2                                                                               PhCH.sub.2                                                                               (+)-pin                                 1377                                                                              OMe           1 PhCH.sub.2                                                                               Ph(CH.sub.2).sub.2                                                                       (+)-pin                                 1378                                                                              OMe           1 PhCH.sub.2                                                                               3-NO.sub.2Ph                                                                             (+)-pin                                 1379                                                                              OMe           1 PhCH.sub.2                                                                               4-NO.sub.2Ph                                                                             (+)-pin                                 1380                                                                              OMe           1 PhCH.sub.2                                                                               3-CO.sub.2 HPh                                                                           (+)-pin                                 1381                                                                              OMe           1 PhCH.sub.2                                                                               4-CO.sub.2 HPh                                                                           (+)-pin                                 1382                                                                              OMe           1 PhCH.sub.2                                                                               3-CN.sub.4 HPh                                                                           (+)-pin                                 1383                                                                              OMe           1 PhCH.sub.2                                                                               4-CN.sub.4 HPh                                                                           (+)-pin                                 1384                                                                              OMe           1 PhCH.sub.2                                                                               3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1385                                                                              OMe           1 PhCH.sub.2                                                                               4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1386                                                                              OMe           1 PhCH.sub.2                                                                               H         OH, OH                                  1387                                                                              OMe           1 PhCH.sub.2                                                                               Methyl    OH, OH                                  1388                                                                              OMe           1 PhCH.sub.2                                                                               Ethyl     OH, OH                                  1389                                                                              OMe           1 PhCH.sub.2                                                                               n-Propyl  OH, OH                                  1390                                                                              OMe           1 PhCH.sub.2                                                                               n-Butyl   OH, OH                                  1391                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 SCH.sub.3                                                                       OH, OH                                  1392                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  1393                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  1394                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  1395                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  1396                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  1397                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1398                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  1399                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  1400                                                                              OMe           1 PhCH.sub.2                                                                               CF.sub.3  OH, OH                                  1401                                                                              OMe           1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.3                                                                        OH, OH                                  1402                                                                              OMe           1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  1403                                                                              OMe           1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  1404                                                                              OMe           1 PhCH.sub.2                                                                               F.sub.5Ph OH, OH                                  1405                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  1406                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  1407                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  1408                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  1409                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  1410                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  1411                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 NO.sub.2                                                                        OH, OH                                  1412                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  1413                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  1414                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 OH                                                                              OH, OH                                  1415                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 OH                                                                      OH, OH                                  1416                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 OH                                                                      OH, OH                                  1417                                                                              OMe           1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  1418                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  1419                                                                              OMe           1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  1420                                                                              OMe           1 PhCH.sub.2                                                                               Ph        OH, OH                                  1421                                                                              OMe           1 PhCH.sub.2                                                                               PhCH.sub.2                                                                               OH, OH                                  1422                                                                              OMe           1 PhCH.sub.2                                                                               Ph(CH.sub.2).sub.2                                                                       OH, OH                                  1423                                                                              OMe           1 PhCH.sub.2                                                                               3-NO.sub.2Ph                                                                             OH, OH                                  1424                                                                              OMe           1 PhCH.sub.2                                                                               4-NO.sub.2Ph                                                                             OH, OH                                  1425                                                                              OMe           1 PhCH.sub.2                                                                               3-CO.sub.2 HPh                                                                           OH, OH                                  1426                                                                              OMe           1 PhCH.sub.2                                                                               4-CO.sub.2 HPh                                                                           OH, OH                                  1427                                                                              OMe           1 PhCH.sub.2                                                                               3-CN.sub.4 HPh                                                                           OH, OH                                  1428                                                                              OMe           1 PhCH.sub.2                                                                               4-CN.sub.4 HPh                                                                           OH, OH                                  1429                                                                              OMe           1 PhCH.sub.2                                                                               3-(HOCH.sub.2)Ph                                                                         OH, OH                                  1430                                                                              OMe           1 PhCH.sub.2                                                                               4-(HOCH.sub.2)Ph                                                                         OH, OH                                  1431                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      H         (+)-pin                                                                             AX                                 1432                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      Methyl    (+)-pin                                 1433                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      Ethyl     (+)-pin                                 1434                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      n-Propyl  (+)-pin                                 1435                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      n-Butyl   (+)-pin                                 1436                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 1437                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 1438                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 1439                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 1440                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 1441                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 1442                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN                                                                              (+)-pin                                 1443                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 1444                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 1445                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.3  (+)-pin                                 1446                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.3                                                                        (+)-pin                                 1447                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 1448                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 1449                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      F.sub.5Ph (+)-pin                                 1450                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 1451                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 1452                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 1453                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 1454                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 1455                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 1456                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 NO.sub.2                                                                        (+)-pin                                 1457                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 1458                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 1459                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 OH                                                                              (+)-pin                                                                             CS                                 1460                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 1461                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 1462                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                 1463                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 1464                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 1465                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      Ph        (+)-pin                                 1466                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      PhCH.sub.2                                                                               (+)-pin                                 1467                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      Ph(CH.sub.2).sub.2                                                                       (+)-pin                                                                             AY                                 1468                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      3-NO.sub.2Ph                                                                             (+)-pin                                 1469                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      4-NO.sub.2Ph                                                                             (+)-pin                                 1470                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      3-CO.sub.2 HPh                                                                           (+)-pin                                 1471                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      4-CO.sub.2 HPh                                                                           (+)-pin                                 1472                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      3-CN.sub.4 HPh                                                                           (+)-pin                                 1473                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      4-CN.sub.4 HPh                                                                           (+)-pin                                 1474                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1475                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1476                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      H         (+)-pin                                 1477                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      Methyl    (+)-pin                                 1478                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      Ethyl     (+)-pin                                 1479                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      n-Propyl  (+)-pin                                 1480                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      n-Butyl   (+)-pin                                 1481                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 1482                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 1483                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 1484                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 1485                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 1486                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 1487                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN                                                                              (+)-pin                                 1488                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 1489                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 1490                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.3  (+)-pin                                 1491                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.3                                                                        (+)-pin                                 1492                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 1493                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 1494                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      F.sub.5Ph (+)-pin                                 1495                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 1496                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 1497                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 1498                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 1499                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 1500                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 1501                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 NO.sub.2                                                                        (+)-pin                                 1502                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 1503                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 1504                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 OH                                                                              (+)-pin                                 1505                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 1506                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 1507                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 Me                                                                     (+)-Pin                                 1508                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 1509                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 1510                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      Ph        (+)-pin                                 1511                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      PhCH.sub.2                                                                               (+)-pin                                 1512                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      Ph(CH.sub.2).sub.2                                                                       (+)-pin                                 1513                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      3-NO.sub.2Ph                                                                             (+)-pin                                 1514                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      4-NO.sub.2Ph                                                                             (+)-pin                                 1515                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      3-CO.sub.2 HPh                                                                           (+)-pin                                 1516                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      4-CO.sub.2 HPh                                                                           (+)-pin                                 1517                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      3-CN.sub.4 HPh                                                                           (+)-pin                                 1518                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      4-CN.sub.4 HPh                                                                           (+)-pin                                 1519                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1520                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1521                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      H         OH, OH                                                                              AZ                                 1522                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      Methyl    OH, OH                                  1523                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      Ethyl     OH, OH                                  1524                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      n-Propyl  OH, OH                                  1525                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      n-Butyl   OH, OH                                  1526                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 SCH.sub.3                                                                       OH, OH                                  1527                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  1528                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  1529                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  1530                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  1531                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  1532                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN                                                                              OH, OH                                  1533                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  1534                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  1535                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.3  OH, OH                                  1536                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.3                                                                        OH, OH                                  1537                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  1538                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  1539                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      F.sub.5Ph OH, OH                                  1540                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  1541                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  1542                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  1543                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  1544                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  1545                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  1546                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 NO.sub.2                                                                        OH, OH                                  1547                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  1548                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  1549                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 OH                                                                              OH, OH                                  1550                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 OH                                                                      OH, OH                                  1551                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 OH                                                                      OH, OH                                  1552                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  1553                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  1554                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  1555                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      Ph        OH, OH                                  1556                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      PhCH.sub.2                                                                               OH, OH                                  1557                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      Ph(CH.sub.2).sub.2                                                                       OH, OH                                                                              AJ                                 1558                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      3-NO.sub.2Ph                                                                             OH, OH                                  1559                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      4-NO.sub.2Ph                                                                             OH, OH                                  1560                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      3-CO.sub.2 HPh                                                                           OH, OH                                  1561                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      4-CO.sub.2 HPph                                                                          OH, OH                                  1562                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      3-CN.sub.4 HPh                                                                           OH, OH                                  1563                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      4-CN.sub.4 HPh                                                                           OH, OH                                  1564                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      3-(HOCH.sub.2)Ph                                                                         OH, OH                                  1565                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      4-(HOCH.sub.2)Ph                                                                         OH, OH                                  1566                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      H         OH, OH                                  1567                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      Methyl    OH, OH                                  1568                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      Ethyl     OH, OH                                  1569                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      n-Propyl  OH, OH                                  1570                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      n-Butyl   OH, OH                                  1571                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 SCH.sub.3                                                                       OH, OH                                  1572                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  1573                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  1574                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  1575                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  1576                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  1577                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN                                                                              OH, OH                                  1578                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  1579                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  1580                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.3  OH, OH                                  1581                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.3                                                                        OH, OH                                  1582                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  1583                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  1584                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      F.sub.5Ph OH, OH                                  1585                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  1586                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  1587                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  1588                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  1589                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  1590                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  1591                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 NO.sub.2                                                                        OH, OH                                  1592                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  1593                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  1594                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 OH                                                                              OH, OH                                  1595                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 OH                                                                      OH, OH                                  1596                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 OH                                                                      OH, OH                                  1597                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  1598                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  1599                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  1600                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      Ph        OH, OH                                  1601                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      PhCH.sub.2                                                                               OH, OH                                  1602                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      Ph(CH.sub.2).sub.2                                                                       OH, OH                                  1603                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      3-NO.sub.2Ph                                                                             OH, OH                                  1604                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      4-NO.sub.2Ph                                                                             OH, OH                                  1605                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      3-CO.sub.2 HPh                                                                           OH, OH                                  1606                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      4-CO.sub.2 HPh                                                                           OH, OH                                  1607                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      3-CN.sub.4 HPh                                                                           OH, OH                                  1608                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      4-CN.sub.4 HPh                                                                           OH, OH                                  1609                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      3-(HOCH.sub.2)Ph                                                                         OH, OH                                  1610                                                                              NH(CNH)NH.sub.2                                                                              1 PhCH.sub.2 CH.sub.2                                                                      4-(HOCH.sub.2)-Ph                                                                        OH, OH                                  1611                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      H         (+)-pin                                 1612                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      Methyl    (+)-pin                                 1613                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      Ethyl     (+)-pin                                 1614                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      n-Propyl  (+)-pin                                 1615                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      n-Butyl   (+)-pin                                 1616                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 1617                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 1618                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 1619                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 1620                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 1621                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 1622                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN                                                                              (+)-pin                                 1623                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 1624                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 1625                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.3  (+)-pin                                 1626                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.3                                                                        (+)-pin                                 1627                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 1628                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 1629                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      F.sub.5Ph (+)-pin                                 1630                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 1631                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 1632                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 1633                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 1634                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 1635                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 1636                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 NO.sub.2                                                                        (+)-pin                                 1637                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 1638                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 1639                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub. OH                                                                               (+)-pin                                 1640                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 1641                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 1642                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                 1643                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 1644                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 1645                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      Ph        (+)-pin                                 1646                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      PhCH.sub.2                                                                               (+)-pin                                 1647                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      Ph(CH.sub.2).sub.2                                                                       (+)-pin                                 1648                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      3-NO.sub.2Ph                                                                             (+)-pin                                 1649                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      4-NO.sub.2Ph                                                                             (+)-pin                                 1650                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      3-CO.sub.2 HPh                                                                           (+)-pin                                 1651                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      4-CO.sub.2 HPh                                                                           (+)-pin                                 1652                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      3-CN.sub.4 HPh                                                                           (+)pin                                  1653                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      4-CN.sub.4 HPh                                                                           (+)-pin                                 1654                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1655                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1656                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      H         OH, OH                                  1657                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      Methyl    OH, OH                                  1658                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      Ethyl     OH, OH                                  1659                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      n-Propyl  OH, OH                                  1660                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      n-Butyl   OH, OH                                  1661                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 SCH.sub.3                                                                       OH, OH                                  1662                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  1663                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  1664                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  1665                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  1666                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  1667                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN                                                                              OH, OH                                  1668                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  1669                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  1670                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.3  OH, OH                                  1671                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.3                                                                        OH, OH                                  1672                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  1673                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  1674                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      F.sub.5Ph OH, OH                                  1675                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  1676                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  1677                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  1678                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  1679                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  1680                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  1681                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 NO.sub.2                                                                        OH, OH                                  1682                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  1683                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  1684                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 OH                                                                              OH, OH                                  1685                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 OH                                                                      OH, OH                                  1686                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 OH                                                                      OH, OH                                  1687                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  1688                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  1689                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  1690                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      Ph        OH, OH                                  1691                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      PhCH.sub.2                                                                               OH, OH                                  1692                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      Ph(CH.sub.2).sub.2                                                                       OH, OH                                  1693                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      3-NO.sub.2Ph                                                                             OH, OH                                  1694                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      4-NO.sub.2Ph                                                                             OH, OH                                  1695                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      3-CO.sub.2 HPh                                                                           OH, OH                                  1696                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      4-CO.sub.2 HPh                                                                           OH, OH                                  1697                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      3-CN.sub.4 HPh                                                                           OH, OH                                  1698                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      4-CN.sub.4 HPh                                                                           OH, OH                                  1699                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      3-(HOCH.sub.2)Ph                                                                         OH, OH                                  1700                                                                              S(CNH)NH.sub.2                                                                               1 PhCH.sub.2 CH.sub.2                                                                      4-(HOCH.sub.2)Ph                                                                         OH, OH                                  1701                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      H         (+)-pin                                 1702                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      Methyl    (+)-pin                                 1703                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      Ethyl     (+)-pin                                 1704                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      n-Propyl  (+)-pin                                 1705                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      n-Butyl   (+)-pin                                 1706                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 1707                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 1708                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 1709                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 1710                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 1711                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 1712                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN                                                                              (+)-pin                                 1713                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 1714                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 1715                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.3  (+)-pin                                 1716                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.3                                                                        (+)-pin                                 1717                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 1718                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 1719                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      F.sub.5Ph (+)-pin                                 1720                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 1721                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 1722                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 1723                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 1724                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 1725                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 1726                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 NO.sub.2                                                                        (+)-pin                                 1727                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 1728                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 1729                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 OH                                                                              (+)-pin                                 1730                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 1731                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 1732                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                 1733                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 1734                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 1735                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      Ph        (+)-pin                                 1736                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      PhCH.sub.2                                                                               (+)-pin                                 1737                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      Ph(CH.sub.2).sub.2                                                                       (+)-pin                                 1738                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      3-NO.sub.2Ph                                                                             (+)-pin                                 1739                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      4-NO.sub.2Ph                                                                             (+)-pin                                 1740                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      3-CO.sub.2 HPh                                                                           (+)-pin                                 1741                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      4-CO.sub.2 HPh                                                                           (+)-pin                                 1742                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      3-CN.sub.4 HPh                                                                           (+)-pin                                 1743                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      4-CN.sub.4 HPh                                                                           (+)-pin                                 1744                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1745                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1746                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      H         OH, OH                                  1747                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      Methyl    OH, OH                                  1748                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      Ethyl     OH, OH                                  1749                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      n-Propyl  OH, OH                                  1750                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      n-Butyl   OH, OH                                  1751                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 SCH.sub.3                                                                       OH, OH                                  1752                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  1753                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  1754                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  1755                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  1756                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  1757                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN                                                                              OH, OH                                  1758                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  1759                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  1760                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.3  OH, OH                                  1761                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.3                                                                        OH, OH                                  1762                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  1763                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  1764                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      F.sub.5Ph OH, OH                                  1765                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  1766                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  1767                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  1768                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  1769                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  1770                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  1771                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 NO.sub.2                                                                        OH, OH                                  1772                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  1773                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  1774                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 OH                                                                              OH, OH                                  1775                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 OH                                                                      OH, OH                                  1776                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 OH                                                                      OH, OH                                  1777                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  1778                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  1779                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  1780                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      Ph        OH, OH                                  1781                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      PhCH.sub.2                                                                               OH, OH                                  1782                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      Ph(CH.sub.2).sub.2                                                                       OH, OH                                  1783                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      3-NO.sub.2Ph                                                                             OH, OH                                  1784                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      4-NO.sub.2Ph                                                                             OH, OH                                  1785                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      3-CO.sub.2 HPh                                                                           OH, OH                                  1786                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      4-CO.sub.2 HPh                                                                           OH, OH                                  1787                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      3-CN.sub.4 HPh                                                                           OH, OH                                  1788                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      4-CN.sub.4 HPh                                                                           OH, OH                                  1789                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      3-(HOCH.sub.2)Ph                                                                         OH, OH                                  1790                                                                              OMe           1 PhCH.sub.2 CH.sub.2                                                                      4-(HOCH.sub.2)Ph                                                                         OH, OH                                  1791                                                                              NH(CNH)H      1 Ph        H         (+)-pin                                 1792                                                                              NH(CNH)H      1 Ph        Methyl    (+)-pin                                 1793                                                                              NH(CNH)H      1 Ph        Ethyl     (+)-pin                                 1794                                                                              NH(CNH)H      1 Ph        n-Propyl  (+)-pin                                 1795                                                                              NH(CNH)H      1 Ph        n-Butyl   (+)-pin                                 1796                                                                              NH(CNH)H      1 Ph        CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 1797                                                                              NH(CNH)H      1 Ph        CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 1798                                                                              NH(CNH)H      1 Ph        CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 1799                                                                              NH(CNH)H      1 Ph        CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 1800                                                                              NH(CNH)H      1 Ph        CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 1801                                                                              NH(CNH)H      1 Ph        CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 1802                                                                              NH(CNH)H      1 Ph        CH.sub.2 CN                                                                              (+)-pin                                 1803                                                                              NH(CNH)H      1 Ph        CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 1804                                                                              NH(CNH)H      1 Ph        CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 1805                                                                              NH(CNH)H      1 Ph        CF.sub.3  (+)-pin                                 1806                                                                              NH(CNH)H      1 Ph        CF.sub.2 CF.sub.3                                                                        (+)-pin                                 1807                                                                              NH(CNH)H      1 Ph        CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 1808                                                                              NH(CNH)H      1 Ph        CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 1809                                                                              NH(CNH)H      1 Ph        F.sub.5Ph (+)-pin                                 1810                                                                              NH(CNH)H      1 Ph        CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 1811                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 1812                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 1813                                                                              NH(CNH)H      1 Ph        CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 1814                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 1815                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 1816                                                                              NH(CNH)H      1 Ph        CH.sub.2 NO.sub.2                                                                        (+)-pin                                 1817                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 1818                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 1819                                                                              NH(CNH)H      1 Ph        CH.sub.2 OH                                                                              (+)-Pin                                 1820                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 1821                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 1822                                                                              NH(CNH)H      1 Ph        CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                 1823                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 1824                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 1825                                                                              NH(CNH)H      1 Ph        Ph        (+)-pin                                 1826                                                                              NH(CNH)H      1 Ph        PhCH.sub.2                                                                               (+)-pin                                 1827                                                                              NH(CNH)H      1 Ph        Ph(CH.sub.2).sub.2                                                                       (+)-pin                                 1828                                                                              NH(CNH)H      1 Ph        3-NO.sub.2Ph                                                                             (+)-pin                                 1829                                                                              NH(CNH)H      1 Ph        4-NO.sub.2Ph                                                                             (+)-Pin                                 1830                                                                              NH(CNH)H      1 Ph        3-CO.sub.2 HP                                                                            (+)-pin                                 1831                                                                              NH(CNH)H      1 Ph        4-CO.sub.2 HPh                                                                           (+)-pin                                 1832                                                                              NH(CNH)H      1 Ph        3-CN.sub.4 HPh                                                                           (+)-pin                                 1833                                                                              NH(CNH)H      1 Ph        4-CN.sub.4 HPh                                                                           (+)-pin                                 1834                                                                              NH(CNH)H      1 Ph        3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1835                                                                              NH(CNH)H      1 Ph        4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1836                                                                              NH(CNH)H      1 Ph        H         OH, OH                                  1837                                                                              NH(CNH)H      1 Ph        Methyl    OH, OH                                  1838                                                                              NH(CNH)H      1 Ph        Ethyl     OH, OH                                  1839                                                                              NH(CNH)H      1 Ph        n-Propyl  OH, OH                                  1840                                                                              NH(CNH)H      1 Ph        n-Butyl   OH, OH                                  1841                                                                              NH(CNH)H      1 Ph        CH.sub.2 SCH.sub.3                                                                       OH, OH                                  1842                                                                              NH(CNH)H      1 Ph        CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  1843                                                                              NH(CNH)H      1 Ph        CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  1844                                                                              NH(CNH)H      1 Ph        CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  1845                                                                              NH(CNH)H      1 Ph        CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  1846                                                                              NH(CNH)H      1 Ph        CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  1847                                                                              NH(CNH)H      1 Ph        CH.sub.2 CN                                                                              OH, OH                                  1848                                                                              NH(CNH)H      1 Ph        CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  1849                                                                              NH(CNH)H      1 Ph        CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  1850                                                                              NH(CNH)H      1 Ph        CF.sub.3  OH, OH                                  1851                                                                              NH(CNH)H      1 Ph        CF.sub.2 CF.sub.3                                                                        OH, OH                                  1852                                                                              NH(CNH)H      1 Ph        CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  1853                                                                              NH(CNH)H      1 Ph        CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  1854                                                                              NH(CNH)H      1 Ph        F.sub.5Ph OH, OH                                  1855                                                                              NH(CNH)H      1 Fh        CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  1856                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  1857                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  1858                                                                              NH(CNH)H      1 Ph        CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  1858                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  1860                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  1861                                                                              NH(CNH)H      1 Ph        CH.sub.2 NO.sub.2                                                                        OH, OH                                  1862                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  1863                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  1864                                                                              NH(CNH)H      1 Ph        CH.sub.2 OH                                                                              OH, OH                                  1865                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.2 OH                                                                      OH, OH                                  1866                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.3 OH                                                                      OH, OH                                  1867                                                                              NH(CNH)H      1 Ph        CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  1868                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  1869                                                                              NH(CNH)H      1 Ph        (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  1870                                                                              NH(CNH)H      1 Ph        Ph        OH, OH                                  1871                                                                              NH(CNH)H      1 Ph        PhCH.sub.2                                                                               OH, OH                                  1872                                                                              NH(CNH)H      1 Ph        Ph(CH.sub.2).sub.2                                                                       OH, OH                                  1873                                                                              NH(CNH)H      1 Ph        3-NO.sub.2Ph                                                                             OH, OH                                  1874                                                                              NH(CNH)H      1 Ph        4-NO.sub.2Ph                                                                             OH, OH                                  1875                                                                              NH(CNH)H      1 Ph        3-CO.sub.2 HPh                                                                           OH, OH                                  1876                                                                              NH(CNH)H      1 Ph        4-CO.sub.2 HPh                                                                           OH, OH                                  1877                                                                              NH(CNH)H      1 Ph        3-CN.sub.4 HPh                                                                           OH, OH                                  1878                                                                              NH(CNH)H      1 Ph        4-CN.sub.4 HPh                                                                           OH, OH                                  1879                                                                              NH(CNH)H      1 Ph        3-(HOCH.sub.2)Ph                                                                         OH, OH                                  1880                                                                              NH(CNH)H      1 Ph        4-(HOCH.sub.2)Ph                                                                         OH, OH                                  1881                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               H         (+)-pin                                 1882                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               Methyl    (+)-pin                                 1883                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               Ethyl     (+)-pin                                 1884                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               n-Propyl  (+)-pin                                 1885                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               n-Butyl   (+)-pin                                 1886                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 1887                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 1888                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 1889                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 1890                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 1891                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 1892                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                 1893                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 1894                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 1895                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CF.sub.3  (+)-pin                                 1896                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.3                                                                        (+)-pin                                 1897                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 1898                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 1899                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               F.sub.5Ph (+)-pin                                 1900                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 1901                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 1902                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 1903                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 1904                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 1905                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 1906                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 NO.sub.2                                                                        (+)-pin                                 1907                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 1908                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 1909                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 OH                                                                              (+)-pin                                 1910                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 1911                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 1912                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                 1913                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 1914                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 1915                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               Ph        (+)-pin                                 1916                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               PhCH.sub.2                                                                               (+)-pin                                 1917                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               Ph(CH.sub.2).sub.2                                                                       (+)-pin                                 1918                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               3-NO.sub.2Ph                                                                             (+)-pin                                 1919                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               4-NO.sub.2Ph                                                                             (+)-pin                                 1920                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               3-CO.sub.2 HPh                                                                           (+)-pin                                 1921                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               4-CO.sub.2 HPh                                                                           (+)-pin                                 1922                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               3-CN.sub.4 HPh                                                                           (+)-pin                                 1923                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               4-CN.sub.4 HPh                                                                           (+)-pin                                 1924                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1925                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 1926                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               H         OH, OH                                  1927                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               Methyl    OH, OH                                  1928                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               Ethyl     OH, OH                                  1929                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               n-Propyl  OH, OH                                  1930                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               n-Butyl   OH, OH                                  1931                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 SCH.sub.3                                                                       OH, OH                                  1932                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  1933                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  1934                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  1935                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  1936                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  1937                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              OH, OH                                  1938                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  1939                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  1940                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CF.sub.3  OH, OH                                  1941                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.3                                                                        OH, OH                                  1942                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  1943                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  1944                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               F.sub.5Ph OH, OH                                  1945                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  1946                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  1947                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  1948                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  1949                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  1950                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  1951                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 NO.sub.2                                                                        OH, OH                                  1952                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  1953                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  1954                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 OH                                                                              OH, OH                                  1955                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 OH                                                                      OH, OH                                  1956                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 OH                                                                      OH, OH                                  1957                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  1958                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  1959                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  1960                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               Ph        OH, OH                                  1961                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               PhCH.sub.2                                                                               OH, OH                                  1962                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               Ph(CH.sub.2).sub.2                                                                       OH, OH                                  1963                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               3-NO.sub.2Ph                                                                             OH, OH                                  1964                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               4-NO.sub.2Ph                                                                             OH, OH                                  1965                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               3-CO.sub.2 HPh                                                                           OH, OH                                  1966                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               4-CO.sub.2 HPh                                                                           OH, OH                                  1967                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               3-CN.sub.4 HPh                                                                           OH, OH                                  1968                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               4-CN.sub.4 HPh                                                                           OH, OH                                  1969                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               3-(HOCH.sub.2)Ph                                                                         OH, OH                                  1970                                                                              NH(CNH)H      1 PhCH.sub.2                                                                               4-(HOCH.sub.2)Ph                                                                         OH, OH                                  1971                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      H         (+)-pin                                 1972                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      Methyl    (+)-pin                                 1973                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      Ethyl     (+)-pin                                 1974                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      n-Propyl  (+)-pin                                 1875                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      n-Butyl   (+)-pin                                 1976                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 SCH.sub.3                                                                       (+)-pin                                 1977                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                 1978                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                 1979                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                 1980                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                 1981                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                 1982                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN                                                                              (+)-pin                                 1983                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                 1984                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                 1985                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.3  (+)-pin                                 1986                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.3                                                                        (+)-pin                                 1987                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                 1988                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                 1989                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      F.sub.5Ph (+)-pin                                 1990                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                 1991                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                 1992                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                 1993                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                 1994                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                 1995                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                 1996                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 NO.sub.2                                                                        (+)-pin                                 1997                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                 1998                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                 1999                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 OH                                                                              (+)-pin                                 2000                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 OH                                                                      (+)-pin                                 2001                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 OH                                                                      (+)-pin                                 2002                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                 2003                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                 2004                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                 2005                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      Ph        (+)-pin                                 2006                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      PhCH.sub.2                                                                               (+)-pin                                 2007                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      Ph(CH.sub.2).sub.2                                                                       (+)-pin                                 2008                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      3-NO.sub.2Ph                                                                             (+)-pin                                 2009                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      4-NO.sub.2Ph                                                                             (+)-pin                                 2010                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      3-CO.sub.2 HPh                                                                           (+)-pin                                 2011                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      4-CO.sub.2 HPh                                                                           (+)-pin                                 2012                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      3-CN.sub.4 HPh                                                                           (+)-pin                                 2013                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      4-CN.sub.4 HPh                                                                           (+)-pin                                 2014                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      3-(HOCH.sub.2)Ph                                                                         (+)-pin                                 2015                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      4-(HOCH.sub.2)Ph                                                                         (+)-pin                                 2016                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      H         OH, OH                                  2017                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      Methyl    OH, OH                                  2018                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      Ethyl     OH, OH                                  2019                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      n-Propyl  OH, OH                                  2020                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      n-Butyl   OH, OH                                  2021                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 SCH.sub.3                                                                       OH, OH                                  2022                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                  2023                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                  2024                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                  2025                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                  2026                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                  2027                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN                                                                              OH, OH                                  2028                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                  2029                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                  2030                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.3  OH, OH                                  2031                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.3                                                                        OH, OH                                  2032                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                  2033                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                  2034                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      F.sub.5Ph OH, OH                                  2035                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 H                                                                      OH, OH                                  2036                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                  2037                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                  2038                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CN.sub.4 H                                                                      OH, OH                                  2039                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                  2040                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                  2041                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 NO.sub.2                                                                        OH, OH                                  2042                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                  2043                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                  2044                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 OH                                                                              OH, OH                                  2045                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 OH                                                                      OH, OH                                  2046                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 OH                                                                      OH, OH                                  2047                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                  2048                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                  2049                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                  2050                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      Ph        OH, OH                                  2051                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      PhCH.sub.2                                                                               OH, OH                                  2052                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      Ph(CH.sub.2).sub.2                                                                       OH, OH                                  2053                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      3-NO.sub.2Ph                                                                             OH, OH                                  2054                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      4-NO.sub.2Ph                                                                             OH, OH                                  2055                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      3-CO.sub.2 HPh                                                                           OH, OH                                  2056                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      4-CO.sub.2 HPh                                                                           OH, OH                                  2057                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      3-CN.sub.4 HPh                                                                           OH, OH                                  2058                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      4-CN.sub.4 HPh                                                                           OH, OH                                  2059                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      3-(HOCH.sub.2)Ph                                                                         OH, OH                                  2060                                                                              NH(CNH)H      1 PhCH.sub.2 CH.sub.2                                                                      4-(HOCH.sub.2)Ph                                                                         OH, OH                                  2061                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               3-NO.sub.2Ph                                                                             (+)-pin                                                                             CU                                 2062                                                                              NH(CNH)NH.sub.2                                                                              1 Ph        PhCH.sub.2                                                                               (+)-pin                                 2063                                                                              NH(CNH)NH.sub.2                                                                              1 Ph        PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                 2064                                                                              S(CNH)NH.sub.2                                                                               1 Ph        PhCH.sub.2                                                                               (+)-pin                                 2065                                                                              S(CNH)NH.sub.2                                                                               1 Ph        PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                 2066                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN                                                                              (+)-pin                                                                             CN                                 2067                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2                                                                               CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                                                             CO                                 2068                                                                              CH.sub.2 NH.sub.2                                                                            1 PhCH.sub.2 CH.sub.2                                                                      CH.sub.2 OCH.sub.2 Ph                                                                    (+)-pin                                                                             CT                                 __________________________________________________________________________      AG. Anal. calcd. for C.sub.32 H.sub.42 BN.sub.5 O.sub.3.0.7 H.sub.2 O.1.7      HCl: C, 61.00; H, 7.21; Cl, 9.56 N, 11.11. Found: C, 60.93; H, 7.20; Cl,       9.57 N, 11.55.                                                                 AH. Anal. calcd. for C.sub.22 H.sub.28 BN.sub.5 O.sub.3.12H.sub.2              O.2.6HCl: C, 36.09; Cl., 12.59; N, 9.56. Found: C, 36.25; Cl, 12.52; N,        9.32.                                                                          AI. Anal. calcd. for C.sub.16 H.sub.24 BN.sub.5 O.sub.3.1.5 H.sub.2 O.1.8      HCl: C, 43.89; H, 6.63; Cl, 14.57; N, 16.06. Found: C, 44.01; H, 6.28; Cl      14.21; N, 15.59.                                                               AJ. Anal. calcd. for C.sub.25 H.sub.34 BN.sub.5 O.sub.3.2 H.sub.2 O.1.6        HCl: C, 53.84; H, 7.16; Cl, 10.17; N, 12.56. Found: C, 53.71; H, 7.13; Cl      10.25; N, 12.60.                                                               AK. MS (M + H).sup.+: Calc. 480, Found 480.                                    AL. MS (M + H).sup.+: Calc. 494, Found 494.                                    AM. MS (M + H).sup.+: Calc. 522, Found 522.                                    AN MS (M + H).sup.+: Calc. 540, Found 540.                                     AO. MS (M + H).sup.+: Calc. 510, Found 510.                                    AP. MS (M + H).sup.+: Calc. 600, Found 600.                                    AQ. MS (M + H).sup.+: Calc. 556, Found 556.                                    AR. MS (M + H).sup.+: Calc. 570, Found 570.                                    AS. MS (M + H).sup.+: Calc. 601, Found 601.                                    AT. MS (M + H).sup.+: Calc. 598, Found 598.                                    AU. MS (M + H).sup.+: Calc. 629, Found 629.                                    AV. MS (M + H).sup.+: Calc. 422, Found 422.                                    AW. MS (M + H).sup.+: Calc. 538, Found 538.                                    AX. MS (M + H).sup.+: Calc. 494, Found 494.                                    AY. MS (M + H).sup.+: Calc. 598, Found 598.                                    AZ. MS (M + H).sup.+: Calc. 360, Found 360.                                    CN. MS (M + H).sup.+: Calc. 519, Found 519.                                    CO. MS (M + H).sup.+: Calc. 562, Found 562.                                    CP. MS (M + H).sup.+: Calc. 552, Found 552.                                    CQ. MS (M + H).sup.+: Calc. 571, Found 571.                                    CR. MS (M + H).sup.+: Calc. 520, Found 520.                                    CS. MS (M + H).sup.+: Calc. 524, Found 524.                                    CT. MS (M + H).sup.+: Calc. 614, Found 614.                                    CU. MS (M + H).sup.+: Calc. 571, Found 571.                              

                                      TABLE 15                                     __________________________________________________________________________      ##STR110##                                                                                                        Phys                                       Ex.                                                                               X         m R.sup.13                                                                             R.sup.14  Y.sup.1 Y.sup.2                                                                     Data                                       __________________________________________________________________________     2073                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    H         (+)-pin                                                                             BW                                         2074                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    Methyl    (+)-pin                                                                             BX                                         2075                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    Ethyl     (+)-pin                                         2076                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    n-Propyl  (+)-pin                                         2077                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    n-Butyl   (+)-pin                                         2078                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         2079                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         2080                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         2081                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         2082                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         2083                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         2084                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CN                                                                              (+)-pin                                         2085                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         2086                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         2087                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.3  (+)-pin                                         2088                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.2 CF.sub.3                                                                        (+)-pin                                         2089                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         2090                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         2091                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    F.sub.5 Ph                                                                               (+)-pin                                         2092                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         2093                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         2094                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         2095                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         2096                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         2097                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         2098                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 NO.sub.2                                                                        (+)-pin                                         2099                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         2100                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         2101                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 OH                                                                              (+)-pin                                         2102                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         2103                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         2104                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         2105                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         2106                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         2107                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-NO.sub.2 Ph                                                                            (+)-pin                                         2108                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-NO.sub.2 Ph                                                                            (+)-pin                                         2109                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-CO.sub.2 HPh                                                                           (+)-pin                                         2110                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-CO.sub.2 HPh                                                                           (+)-pin                                         2111                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-CN.sub.4 HPh                                                                           (+)-pin                                         2112                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-CN.sub.4 HPh                                                                           (+)-pin                                         2113                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2114                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2115                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    H         (+)-pin                                         2116                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    Methyl    (+)-pin                                         2117                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    Ethyl     (+)-pin                                         2118                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    n-Propyl  (+)-pin                                         2119                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    n-Butyl   (+)-pin                                         2120                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         2121                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         2122                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         2123                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         2124                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         2125                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         2126                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CN                                                                              (+)-pin                                         2127                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         2128                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         2129                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.3  (+)-pin                                         2130                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.3                                                                        (+)-pin                                         2131                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         2132                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         2133                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    F.sub.5 Ph                                                                               (+)-pin                                         2134                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         2135                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         2136                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         2137                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         2138                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         2139                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         2140                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 NO.sub.2                                                                        (+)-pin                                         2141                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         2142                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         2143                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 OH                                                                              (+)-pin                                         2144                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         2145                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         2146                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         2147                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         2148                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         2149                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-NO.sub.2 Ph                                                                            (+)-pin                                         2150                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-NO.sub.2 Ph                                                                            (+)-pin                                         2151                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-CO.sub.2 HPh                                                                           (+)-pin                                         2152                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-CO.sub.2 HPh                                                                           (+)-pin                                         2153                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-CN.sub.4 HPh                                                                           (+)-pin                                         2154                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-CN.sub.4 HPh                                                                           (+)-pin                                         2155                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2156                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2157                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    H         OH, OH                                          2158                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    Methyl    OH, OH                                          2159                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    Ethyl     OH, OH                                          2160                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    n-Propyl  OH, OH                                          2161                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    n-Butyl   OH, OH                                          2162                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 SCH.sub.3                                                                       OH, OH                                          2163                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          2164                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          2165                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          2166                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          2167                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          2168                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CN                                                                              OH, OH                                          2169                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          2170                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          2171                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.3  OH, OH                                          2172                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.2 CF.sub.3                                                                        OH, OH                                          2173                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          2174                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          2175                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    F.sub.5 Ph                                                                               OH, OH                                          2176                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          2177                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          2178                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          2179                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          2180                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          2181                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          2182                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 NO.sub.2                                                                        OH, OH                                          2183                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          2184                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          2185                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 OH                                                                              OH, OH                                          2186                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 OH                                                                      OH, OH                                          2187                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 OH                                                                      OH, OH                                          2188                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          2189                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          2190                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          2191                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-NO.sub.2 Ph                                                                            OH, OH                                          2192                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-NO.sub.2 Ph                                                                            OH, OH                                          2193                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-CO.sub.2 HPh                                                                           OH, OH                                          2194                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-CO.sub.2 HPh                                                                           OH, OH                                          2195                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-CN.sub.4 HPh                                                                           OH, OH                                          2196                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-CN.sub.4 HPh                                                                           OH, OH                                          2197                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    3-(HOCH.sub.2)Ph                                                                         OH, OH                                          2198                                                                              CH.sub.2 NH.sub.2                                                                        1 Ph    4-(HOCH.sub.2)Ph                                                                         OH, OH                                          2199                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    H         OH, OH                                          2200                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    Methyl    OH, OH                                          2201                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    Ethyl     OH, OH                                          2202                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    n-Propyl  OH, OH                                          2203                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    n-Butyl   OH, OH                                          2204                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 SCH.sub.3                                                                       OH, OH                                          2205                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 (SO)CH.sub.3                                                                    OH,CH                                           2206                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          2207                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          2208                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          2209                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          2210                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CN                                                                              OH, OH                                          2211                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          2212                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          2213                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.3  OH, OH                                          2214                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.3                                                                        OH, OH                                          2215                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          2216                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          2217                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    F.sub.5 Ph                                                                               OH, OH                                          2218                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          2219                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          2220                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          2221                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          2222                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          2223                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          2224                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 NO.sub.2                                                                        OH, OH                                          2225                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          2226                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          2227                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 OH                                                                              OH, OH                                          2228                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 OH                                                                      OH, OH                                          2229                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 OH                                                                      OH, OH                                          2230                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          2231                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          2232                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          2233                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-NO.sub.2 Ph                                                                            OH, OH                                          2234                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-NO.sub.2 Ph                                                                            OH, OH                                          2235                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-CO.sub.2 HPh                                                                           OH, OH                                          2236                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-CO.sub.2 HPh                                                                           OH, OH                                          2237                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-CN.sub.4 HPh                                                                           OH, OH                                          2238                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-CN.sub.4 HPh                                                                           OH, OH                                          2239                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    3-(HOCH.sub.2)Ph                                                                         OH, OH                                          2240                                                                              NH(CNH)NH.sub.2                                                                          1 Ph    4-(HOCH.sub.2)Ph                                                                         OH, OH                                          2241                                                                              S(CNH)NH.sub.2                                                                           1 Ph    H         (+)-pin                                         2242                                                                              S(CNH)NH.sub.2                                                                           1 Ph    Methyl    (+)-pin                                         2243                                                                              S(CNH)NH.sub.2                                                                           1 Ph    Ethyl     (+)-pin                                         2244                                                                              S(CNH)NH.sub.2                                                                           1 Ph    n-Propyl  (+)-pin                                         2245                                                                              S(CNH)NH.sub.2                                                                           1 Ph    n-Butyl   (+)-pin                                         2246                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         2247                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         2248                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         2249                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         2250                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         2251                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         2252                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CN                                                                              (+)-pin                                         2253                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         2254                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         2255                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.3  (+)-pin                                         2256                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.2 CF.sub.3                                                                        (+)-pin                                         2257                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         2258                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         2259                                                                              S(CNH)NH.sub.2                                                                           1 Ph    F.sub.5 Ph                                                                               (+)-pin                                         2260                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         2261                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         2262                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         2263                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         2264                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         2265                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         2266                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 NO.sub.2                                                                        (+)-pin                                         2267                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         2268                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         2269                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 OH                                                                              (+)-pin                                         2270                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         2271                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         2272                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         2273                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         2274                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         2275                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-NO.sub.2 Ph                                                                            (+)-pin                                         2276                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-NO.sub.2 Ph                                                                            (+)-pin                                         2277                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-CO.sub.2 HPh                                                                           (+)-pin                                         2278                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-CO.sub.2 HPh                                                                           (+)-pin                                         2279                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-CN.sub.4 HPh                                                                           (+)-pin                                         2280                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-CN.sub.4 HPh                                                                           (+)-pin                                         2281                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2282                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2283                                                                              S(CNH)NH.sub.2                                                                           1 Ph    H         OH, OH                                          2284                                                                              S(CNH)NH.sub.2                                                                           1 Ph    Methyl    OH, OH                                          2285                                                                              S(CNH)NH.sub.2                                                                           1 Ph    Ethyl     OH, OH                                          2286                                                                              S(CNH)NH.sub.2                                                                           1 Ph    n-Propyl  OH, OH                                          2287                                                                              S(CNH)NH.sub.2                                                                           1 Ph    n-Butyl   OH, OH                                          2288                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 SCH.sub.3                                                                       OH, OH                                          2289                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          2290                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          2291                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          2292                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          2293                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          2294                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CN                                                                              OH, OH                                          2295                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          2296                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          2297                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.3  OH, OH                                          2298                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.2 CF.sub.3                                                                        OH, OH                                          2299                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          2300                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          2301                                                                              S(CNH)NH.sub.2                                                                           1 Ph    F.sub.5 Ph                                                                               OH, OH                                          2302                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          2303                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          2304                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          2305                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          2306                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          2307                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          2308                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 NO.sub.2                                                                        OH, OH                                          2309                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          2310                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          2311                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 OH                                                                              OH, OH                                          2312                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 OH                                                                      OH, OH                                          2313                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 OH                                                                      OH, OH                                          2314                                                                              S(CNH)NH.sub.2                                                                           1 Ph    CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          2315                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          2316                                                                              S(CNH)NH.sub.2                                                                           1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          2317                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-NO.sub.2 Ph                                                                            OH, OH                                          2318                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-NO.sub.2 Ph                                                                            OH, OH                                          2319                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-CO.sub.2 HPh                                                                           OH, OH                                          2320                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-CO.sub.2 HPh                                                                           OH, OH                                          2321                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-CN.sub.4 HPh                                                                           OH, OH                                          2322                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-CN.sub.4 HPh                                                                           OH, OH                                          2323                                                                              S(CNH)NH.sub.2                                                                           1 Ph    3-(HOCH.sub.2)Ph                                                                         OH, OH                                          2324                                                                              S(CNH)NH.sub.2                                                                           1 Ph    4-(HOCH.sub.2)Ph                                                                         OH, OH                                          2325                                                                              CH.sub.2 NH.sub.2                                                                        2 Ph    H         (+)-pin                                         2326                                                                              CH.sub.2 NH.sub.2                                                                        2 Ph    H         OH, OH                                          2327                                                                              OMe       1 Ph    H         (+)-pin                                         2328                                                                              OMe       1 Ph    Methyl    (+)-pin                                         2329                                                                              OMe       1 Ph    Ethyl     (+)-pin                                         2330                                                                              OMe       1 Ph    n-Propyl  (+)-pin                                         2331                                                                              OMe       1 Ph    n-Butyl   (+)-pin                                         2332                                                                              OMe       1 Ph    CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         2333                                                                              OMe       1 Ph    CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         2334                                                                              OMe       1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         2335                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         2336                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         2337                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         2338                                                                              OMe       1 Ph    CH.sub.2 CN                                                                              (+)-pin                                         2339                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         2340                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         2341                                                                              OMe       1 Ph    CF.sub.3  (+)-pin                                         2342                                                                              OMe       1 Ph    CF.sub.2 CF.sub.3                                                                        (+)-pin                                         2343                                                                              OMe       1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         2344                                                                              OMe       1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         2345                                                                              OMe       1 Ph    F.sub.5 Ph                                                                               (+)-pin                                         2346                                                                              OMe       1 Ph    CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         2347                                                                              OMe       1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         2348                                                                              OMe       1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         2349                                                                              OMe       1 Ph    CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         2350                                                                              OMe       1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         2351                                                                              OMe       1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         2352                                                                              OMe       1 Ph    CH.sub.2 NO.sub.2                                                                        (+)-pin                                         2353                                                                              OMe       1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         2354                                                                              OMe       1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         2355                                                                              OMe       1 Ph    CH.sub.2 OH                                                                              (+)-pin                                         2356                                                                              OMe       1 Ph    (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         2357                                                                              OMe       1 Ph    (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         2358                                                                              OMe       1 Ph    CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         2359                                                                              OMe       1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         2360                                                                              OMe       1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         2361                                                                              OMe       1 Ph    3-NO.sub.2 Ph                                                                            (+)-pin                                         2362                                                                              OMe       1 Ph    4-NO.sub.2 Ph                                                                            (+)-pin                                         2363                                                                              OMe       1 Ph    3-CO.sub.2 HPh                                                                           (+)-pin                                         2364                                                                              OMe       1 Ph    4-CO.sub.2 HPh                                                                           (+)-pin                                         2365                                                                              OMe       1 Ph    3-CN.sub.4 HPh                                                                           (+)-pin                                         2366                                                                              OMe       1 Ph    4-CN.sub.4 HPh                                                                           (+)-pin                                         2367                                                                              OMe       1 Ph    3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2368                                                                              OMe       1 Ph    4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2369                                                                              OMe       1 Ph    H         OH, OH                                          2370                                                                              OMe       1 Ph    Methyl    OH, OH                                          2371                                                                              OMe       1 Ph    Ethyl     OH, OH                                          2372                                                                              OMe       1 Ph    n-Propyl  OH, OH                                          2373                                                                              OMe       1 Ph    n-Butyl   OH, OH                                          2374                                                                              OMe       1 Ph    CH.sub.2 SCH.sub.3                                                                       OH, OH                                          2375                                                                              OMe       1 Ph    CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          2376                                                                              OMe       1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          2377                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          2378                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          2379                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          2380                                                                              OMe       1 Ph    CH.sub.2 CN                                                                              OH, OH                                          2381                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          2382                                                                              OMe       1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          2383                                                                              OMe       1 Ph    CF.sub.3  OH, OH                                          2384                                                                              OMe       1 Ph    CF.sub.2 CF.sub.3                                                                        OH, OH                                          2385                                                                              OMe       1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          2386                                                                              OMe       1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          2387                                                                              OMe       1 Ph    F.sub.5 Ph                                                                               OH, OH                                          2388                                                                              OMe       1 Ph    CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          2389                                                                              OMe       1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          2390                                                                              OMe       1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          2391                                                                              OMe       1 Ph    CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          2392                                                                              OMe       1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          2393                                                                              OMe       1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          2394                                                                              OMe       1 Ph    CH.sub.2 NO.sub.2                                                                        OH, OH                                          2395                                                                              OMe       1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          2396                                                                              OMe       1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          2397                                                                              OMe       1 Ph    CH.sub.2 OH                                                                              OH, OH                                          2398                                                                              OMe       1 Ph    (CH.sub.2).sub.2 OH                                                                      OH, OH                                          2399                                                                              OMe       1 Ph    (CH.sub.2).sub.3 OH                                                                      OH, OH                                          2400                                                                              OMe       1 Ph    CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          2401                                                                              OMe       1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          2402                                                                              OMe       1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          2403                                                                              OMe       1 Ph    3-NO.sub.2 Ph                                                                            OH, OH                                          2404                                                                              OMe       1 Ph    4-NO.sub.2 Ph                                                                            OH, OH                                          2405                                                                              OMe       1 Ph    3-CO.sub.2 HPh                                                                           OH, OH                                          2406                                                                              OMe       1 Ph    4-CO.sub.2 HPh                                                                           OH, OH                                          2407                                                                              OMe       1 Ph    3-CN.sub.4 HPh                                                                           OH, OH                                          2408                                                                              OMe       1 Ph    4-CN.sub.4 HPh                                                                           OH, OH                                          2409                                                                              OMe       1 Ph    3-(HOCH.sub.2)Ph                                                                         OH, OH                                          2410                                                                              OMe       1 Ph    4-(HOCH.sub.2)Ph                                                                         OH, OH                                          2411                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           H         (+)-pin                                                                             BA                                         2412                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           Methyl    (+)-pin                                                                             BC                                         2413                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           Ethyl     (+)-pin                                         2414                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           n-Propyl  (+)-pin                                                                             BD                                         2415                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           n-Butyl   (+)-pin                                         2416                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                       (+)-pin                                                                             BE                                         2417                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         2418                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         2419                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         2420                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         2421                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         2422                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                              (+)-pin                                                                             BF                                         2423                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         2424                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         2425                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.3  (+)-pin                                         2426                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                        (+)-pin                                         2427                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         2428                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         2429                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           F.sub.5 Ph                                                                               (+)-pin                                         2430                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                                                             BG                                         2431                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         2432                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         2433                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         2434                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         2435                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         2436                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                        (+)-pin                                         2437                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         2438                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         2439                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                              (+)-pin                                                                             CV                                         2440                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 OCH.sub.2 Ph                                                                    (+)-pin                                                                             CW                                         2441                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         2442                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         2443                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                                                             CX                                         2444                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         2445                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         2446                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           Ph        (+)-pin                                         2447                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           PhCH.sub.2                                                                               (+)-pin                                         2448                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-NO.sub.2 Ph                                                                            (+)-pin                                         2449                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-NO.sub.2 Ph                                                                            (+)-pin                                         2450                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-CO.sub.2 HPh                                                                           (+)-pin                                         2451                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-CO.sub.2 HPh                                                                           (+)-pin                                         2452                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-CN.sub.4 HPh                                                                           (+)-pin                                         2453                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-CN.sub.4 HPh                                                                           (+)-pin                                         2454                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2455                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2456                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           H         (+)-pin                                         2457                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           Methyl    (+)-pin                                         2458                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           Ethyl     (+)-pin                                         2459                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           n-Propyl  (+)-pin                                         2460                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           n-Butyl   (+)-pin                                         2461                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         2462                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         2463                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         2464                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         2465                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         2466                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         2467                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                              (+)-pin                                         2468                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         2469                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         2470                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.3  (+)-pin                                         2471                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                        (+)-pin                                         2472                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         2473                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         2474                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           F.sub.5 Ph                                                                               (+)-pin                                         2475                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         2476                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         2477                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         2478                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         2479                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         2480                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         2481                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                        (+)-pin                                         2482                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         2483                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         2484                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                              (+)-pin                                         2485                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         2486                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         2487                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         2488                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         2489                                                                              NH(CNH)NH.sub.2                                                                          1 PhCF.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         2490                                                                              NH(CNH)NH.sub.2                                                                          1 PhCP2 Ph        (+)-pin                                         2491                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-NO.sub.2 Ph                                                                            (+)-pin                                                                             CY                                         2492                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-NO.sub.2 Ph                                                                            (+)-pin                                         2493                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-CO.sub.2 HPh                                                                           (+)-pin                                         2494                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-CO.sub.2 HPh                                                                           (+)-pin                                         2495                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-CN.sub.4 HPh                                                                           (+)-pin                                         2496                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-CN.sub.4 HPh                                                                           (+)-pin                                         2497                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2498                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2499                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           H         OH, OH                                                                              BH                                         2500                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           Methyl    OH, OH                                          2501                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           Ethyl     OH, OH                                          2502                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           n-Propyl  OH, OH                                          2503                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           n-Butyl   OH, OH                                          2504                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                       OH, OH                                          2505                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          2506                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          2507                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          2508                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          2509                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          2510                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                              OH, OH                                          2511                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          2512                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          2513                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.3  OH, OH                                          2514                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                        OH, OH                                          2515                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          2516                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          2517                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           F.sub.5 Ph                                                                               OH, OH                                          2518                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          2519                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          2520                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          2521                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          2522                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          2523                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          2524                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                        OH, OH                                          2525                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          2526                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          2527                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                              OH, OH                                          2528                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                      OH, OH                                          2529                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                      OH, OH                                          2530                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          2531                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          2532                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          2533                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           Ph        OH, OH                                          2534                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-NO.sub.2 Ph                                                                            OH, OH                                          2535                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-NO.sub.2 Ph                                                                            OH, OH                                          2536                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-CO.sub.2 HPh                                                                           OH, OH                                          2537                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-CO.sub.2 HPh                                                                           OH, OH                                          2538                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-CN.sub.4 HPh                                                                           OH, OH                                          2539                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-CN.sub.4 HPh                                                                           OH, OH                                          2540                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           3-(HOCH.sub.2)Ph                                                                         OH, OH                                          2541                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2                                                                           4-(HOCH.sub.2)Ph                                                                         OH, OH                                          2542                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           H         OH, OH                                          2543                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           Methyl    OH, OH                                          2544                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           Ethyl     OH, OH                                          2545                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           n-Propyl  OH, OH                                          2546                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           n-Butyl   OH, OH                                          2547                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                       OH, OH                                          2548                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          2549                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          2550                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          2551                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          2552                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          2553                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                              OH, OH                                          2554                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          2555                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          2556                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.3  OH, OH                                          2557                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                        OH, OH                                          2558                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          2559                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          2560                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           F.sub.5 Ph                                                                               OH, OH                                          2561                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          2562                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          2563                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          2564                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          2565                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          2566                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          2567                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                        OH, OH                                          2568                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          2569                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          2570                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                              OH, OH                                          2571                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                      OH, OH                                          2572                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                      OH, OH                                          2573                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          2574                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          2575                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          2576                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-NO.sub.2 Ph                                                                            OH, OH                                          2577                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-NO.sub.2 Ph                                                                            OH, OH                                          2578                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-CO.sub.2 HPh                                                                           OH, OH                                          2579                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-CO.sub.2 HPh                                                                           OH, OH                                          2580                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-CN.sub.4 HPh                                                                           OH, OH                                          2581                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-CN.sub.4 HPh                                                                           OH,CH                                           2582                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           3-(HOCH.sub.2)Ph                                                                         OH, OH                                          2583                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2                                                                           4-(HOCH.sub.2)Ph                                                                         OH, OH                                          2584                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           H         (+)-pin                                         2585                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           Methyl    (+)-pin                                         2586                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           Ethyl     (+)-pin                                         2587                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           n-Propyl  (+)-pin                                         2588                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           n-Butyl   (+)-pin                                         2589                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         2590                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         2591                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         2592                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         2593                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         2594                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         2595                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                              (+)-pin                                         2596                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         2597                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         2598                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.3  (+)-pin                                         2599                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                        (+)-pin                                         2600                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         2601                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         2602                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           F.sub.5 Ph                                                                               (+)-pin                                         2603                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         2604                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         2605                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         2606                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         2607                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         2608                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         2609                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                        (+)-pin                                         2610                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         2611                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         2612                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                              (+)-pin                                         2613                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         2614                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         2615                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         2616                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         2617                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         2618                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-NO.sub.2 Ph                                                                            (+)-pin                                         2619                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-NO.sub.2 Ph                                                                            (+)-pin                                         2620                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-CO.sub.2 HPh                                                                           (+)-pin                                         2621                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-CO.sub.2 HPh                                                                           (+)-pin                                         2622                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-CN.sub.4 HPh                                                                           (+)-pin                                         2623                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-CN.sub.4 HPh                                                                           (+)-pin                                         2624                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2625                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2626                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           H         OH, OH                                          2627                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           Methyl    OH, OH                                          2628                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           Ethyl     OH, OH                                          2629                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           n-Propyl  OH, OH                                          2630                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           n-Butyl   OH, OH                                          2631                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                       OH, OH                                          2632                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          2633                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          2634                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          2635                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          2636                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          2637                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                              OH, OH                                          2638                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          2639                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          2640                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.3  OH, OH                                          2641                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                        OH, OH                                          2642                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          2643                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          2644                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           F.sub.5 Ph                                                                               OH, OH                                          2645                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          2646                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          2647                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          2648                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          2649                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          2650                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          2651                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                        OH, OH                                          2652                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          2653                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          2654                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                              OH, OH                                          2655                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                      OH, OH                                          2656                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                      OH, OH                                          2657                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          2658                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          2659                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          2660                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-NO.sub.2 Ph                                                                            OH, OH                                          2661                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-NO.sub.2 Ph                                                                            OH, OH                                          2662                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-CO.sub.2 HPh                                                                           OH, OH                                          2663                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-CO.sub.2 HPh                                                                           OH, OH                                          2664                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-CN.sub.4 HPh                                                                           OH, OH                                          2665                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-CN.sub.4 HPh                                                                           OH, OH                                          2666                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           3-(HOCH.sub.2)Ph                                                                         OH, OH                                          2667                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2                                                                           4-(HOCH.sub.2)Ph                                                                         OH, OH                                          2668                                                                              OMe       1 PhCH.sub.2                                                                           H         (+)-pin                                         2669                                                                              OMe       1 PhCH.sub.2                                                                           Methyl    (+)-pin                                         2670                                                                              OMe       1 PhCH.sub.2                                                                           Ethyl     (+)-pin                                         2671                                                                              OMe       1 PhCH.sub.2                                                                           n-Propyl  (+)-pin                                         2672                                                                              OMe       1 PhCH.sub.2                                                                           n-Butyl   (+)-pin                                         2673                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         2674                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         2675                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         2676                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         2677                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         2678                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         2679                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                              (+)-pin                                         2680                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         2681                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         2682                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.3  (+)-pin                                         2683                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                        (+)-pin                                         2684                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         2685                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         2686                                                                              OMe       1 PhCH.sub.2                                                                           F.sub.5 Ph                                                                               (+)-pin                                         2687                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         2688                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         2689                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         2690                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         2691                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         2692                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         2693                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                        (+)-pin                                         2694                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         2695                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         2696                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                              (+)-pin                                         2697                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         2698                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         2699                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         2700                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         2701                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         2702                                                                              OMe       1 PhCH.sub.2                                                                           3-NO.sub.2 Ph                                                                            (+)-pin                                         2703                                                                              OMe       1 PhCH.sub.2                                                                           4-NO.sub.2 Ph                                                                            (+)-pin                                         2704                                                                              OMe       1 PhCH.sub.2                                                                           3-CO.sub.2 HPh                                                                           (+)-pin                                         2705                                                                              OMe       1 PhCH.sub.2                                                                           4-CO.sub.2 HPh                                                                           (+)-pin                                         2706                                                                              OMe       1 PhCH.sub.2                                                                           3-CN.sub.4 HPh                                                                           (+)-pin                                         2707                                                                              OMe       1 PhCH.sub.2                                                                           4-CN.sub.4 HPh                                                                           (+)-pin                                         2708                                                                              OMe       1 PhCH.sub.2                                                                           3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2709                                                                              OMe       1 PhCH.sub.2                                                                           4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2710                                                                              OMe       1 PhCH.sub.2                                                                           H         OH, OH                                          2711                                                                              OMe       1 PhCH.sub.2                                                                           Methyl    OH, OH                                          2712                                                                              OMe       1 PhCH.sub.2                                                                           Ethyl     OH, OH                                          2713                                                                              OMe       1 PhCH.sub.2                                                                           n-Propyl  OH, OH                                          2714                                                                              OMe       1 PhCH.sub.2                                                                           n-Butyl   OH, OH                                          2715                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                       OH, OH                                          2716                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          2717                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          2718                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          2719                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          2720                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          2721                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                              OH, OH                                          2722                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          2723                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          2724                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.3  OH, OH                                          2725                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                        OH, OH                                          2726                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          2727                                                                              OMe       1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          2728                                                                              OMe       1 PhCH.sub.2                                                                           F.sub.5 Ph                                                                               OH, OH                                          2729                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          2730                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          2731                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          2732                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          2733                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          2734                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          2735                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                        OH, OH                                          2736                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          2737                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          2738                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                              OH, OH                                          2739                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                      OH, OH                                          2740                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                      OH, OH                                          2741                                                                              OMe       1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          2742                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          2743                                                                              OMe       1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          2744                                                                              OMe       1 PhCH.sub.2                                                                           3-NO.sub.2 Ph                                                                            OH, OH                                          2745                                                                              OMe       1 PhCH.sub.2                                                                           4-NO.sub.2 Ph                                                                            OH, OH                                          2746                                                                              OMe       1 PhCH.sub.2                                                                           3-CO.sub.2 HPh                                                                           OH, OH                                          2747                                                                              OMe       1 PhCH.sub.2                                                                           4-CO.sub.2 HPh                                                                           OH, OH                                          2748                                                                              OMe       1 PhCH.sub.2                                                                           3-CN.sub.4 HPh                                                                           OH, OH                                          2749                                                                              OMe       1 PhCH.sub.2                                                                           4-CN.sub.4 HPh                                                                           OH, OH                                          2750                                                                              OMe       1 PhCH.sub.2                                                                           3-(HOCH.sub.2)Ph                                                                         OH, OH                                          2751                                                                              OMe       1 PhCH.sub.2                                                                           4-(HOCH.sub.2)Ph                                                                         OH, OH                                          2752                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  H         (+)-pin                                                                             BI                                         2753                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  Methyl    (+)-pin                                         2754                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  Ethyl     (+)-pin                                         2755                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl  (+)-pin                                         2756                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl   (+)-pin                                         2757                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         2758                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         2759                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         2760                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         2761                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         2762                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         2763                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                              (+)-pin                                         2764                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         2765                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         2766                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3  (+)-pin                                         2767                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                        (+)-pin                                         2768                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         2769                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         2770                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 Ph                                                                               (+)-pin                                         2771                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         2772                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         2773                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         2774                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         2775                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         2776                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         2777                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                        (+)-pin                                         2778                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         2779                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         2780                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                              (+)-pin                                                                             CZ                                         2781                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OCH.sub.2 Ph                                                                    (+)-pin                                                                             CA                                         2782                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         2783                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         2784                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         2785                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         2786                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         2787                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 Ph                                                                            (+)-pin                                         2788                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 Ph                                                                            (+)-pin                                         2789                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 HPh                                                                           (+)-pin                                         2790                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 HPh                                                                           (+)-pin                                         2791                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 HPh                                                                           (+)-pin                                         2792                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 HPh                                                                           (+)-pin                                         2793                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2794                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2795                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  H         (+)-pin                                         2796                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  Methyl    (+)-pin                                         2797                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  Ethyl     (+)-pin                                         2798                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl  (+)-pin                                         2799                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl   (+)-pin                                         2800                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         2801                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         2802                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         2803                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         2804                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         2805                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         2806                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                              (+)-pin                                         2807                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         2808                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         2809                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3  (+)-pin                                         2810                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                        (+)-pin                                         2811                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         2812                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         2813                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 Ph                                                                               (+)-pin                                         2814                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         2815                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         2816                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         2817                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         2818                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         2819                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         2820                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                        (+)-pin                                         2821                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         2822                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         2823                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                              (+)-pin                                         2824                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         2825                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         2826                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         2827                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         2828                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         2829                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 Ph                                                                            (+)-pin                                         2830                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 Ph                                                                            (+)-pin                                         2831                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 HPh                                                                           (+)-pin                                         2832                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 HPh                                                                           (+)-pin                                         2833                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 HPh                                                                           (+)-pin                                         2834                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 HPh                                                                           (+)-pin                                         2835                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2836                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2837                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  H         OH, OH                                                                              BJ                                         2838                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  Methyl    OH, OH                                          2839                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  Ethyl     OH, OH                                          2840                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl  OH, OH                                          2841                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl   OH, OH                                          2842                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                       OH, OH                                          2843                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          2844                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          2845                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          2846                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          2847                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          2848                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                              OH, OH                                          2849                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          2850                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          2851                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3  OH, OH                                          2852                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                        OH, OH                                          2853                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          2854                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          2855                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 Ph                                                                               OH, OH                                          2856                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          2857                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          2858                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          2859                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          2860                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          2861                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          2862                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                        OH, OH                                          2863                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          2864                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          2865                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                              OH, OH                                          2866                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                      OH, OH                                          2867                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                      OH, OH                                          2868                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          2869                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          2870                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          2871                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 Ph                                                                            OH, OH                                          2872                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 Ph                                                                            OH, OH                                          2873                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 HPh                                                                           OH, OH                                          2874                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 HPh                                                                           OH, OH                                          2875                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 HPh                                                                           OH, OH                                          2876                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 HPh                                                                           OH, OH                                          2877                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)Ph                                                                         OH, OH                                          2878                                                                              CH.sub.2 NH.sub.2                                                                        1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)Ph                                                                         OH, OH                                          2879                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  B         OH, OH                                          2880                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  Methyl    OH, OH                                          2881                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  Ethyl     OH, OH                                          2882                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl  OH, OH                                          2883                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl   OH, OH                                          2884                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                       OH, OH                                          2885                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          2886                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          2887                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          2888                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          2889                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          2890                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                              OH, OH                                          2891                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          2892                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          2893                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3  OH, OH                                          2894                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                        OH, OH                                          2895                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          2896                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          2897                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 Ph                                                                               OH, OH                                          2898                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          2899                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          2900                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          2901                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          2902                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          2903                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          2904                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                        OH, OH                                          2905                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          2906                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          2907                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                              OH, OH                                          2908                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                      OH, OH                                          2909                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                      OH, OH                                          2910                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          2911                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          2912                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          2913                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 Ph                                                                            OH, OH                                          2914                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 Ph                                                                            OH, OH                                          2915                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 HPh                                                                           OH, OH                                          2916                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 HPh                                                                           OH, OH                                          2917                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 HPh                                                                           OH, OH                                          2918                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 HPh                                                                           OH, OH                                          2919                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)Ph                                                                         OH, OH                                          2920                                                                              NH(CNH)NH.sub.2                                                                          1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)Ph                                                                         OH, OH                                          2921                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  H         (+)-pin                                         2922                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  Methyl    (+)-pin                                         2923                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  Ethyl     (+)-pin                                         2924                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl  (+)-pin                                         2925                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl   (+)-pin                                         2926                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         2927                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         2928                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         2929                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         2930                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         2931                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         2932                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                              (+)-pin                                         2933                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         2934                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         2935                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3  (+)-pin                                         2936                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                        (+)-pin                                         2937                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         2938                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         2939                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 Ph                                                                               (+)-pin                                         2940                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         2941                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         2942                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         2943                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         2944                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         2945                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         2946                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                        (+)-pin                                         2947                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         2948                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         2949                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                              (+)-pin                                         2950                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         2951                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         2952                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         2953                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         2954                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         2955                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 Ph                                                                            (+)-pin                                         2956                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 Ph                                                                            (+)-pin                                         2957                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 HPh                                                                           (+)-pin                                         2958                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 HPh                                                                           (+)-pin                                         2959                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 HPh                                                                           (+)-pin                                         2960                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 HPh                                                                           (+)-pin                                         2961                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2962                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         2963                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  H         OH, OH                                          2964                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  Methyl    OH, OH                                          2965                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  Ethyl     OH, OH                                          2966                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl  OH, OH                                          2967                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl   OH, OH                                          2968                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                       OH, OH                                          2969                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          2970                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          2971                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          2972                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          2973                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          2974                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                              OH, OH                                          2975                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          2976                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          2977                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3  OH, OH                                          2978                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                        OH, OH                                          2979                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          2980                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          2981                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 Ph                                                                               OH, OH                                          2982                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          2983                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          2984                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          2985                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          2986                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          2987                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          2988                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                        OH, OH                                          2989                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          2990                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          2991                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                              OH, OH                                          2992                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                      OH, OH                                          2993                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                      OH, OH                                          2994                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          2995                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          2996                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          2997                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 Ph                                                                            OH, OH                                          2998                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 Ph                                                                            OH, OH                                          2999                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 HPh                                                                           OH, OH                                          3000                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 HPh                                                                           OH, OH                                          3001                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 HPh                                                                           OH, OH                                          3002                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 HPh                                                                           OH, OH                                          3003                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)Ph                                                                         OH, OH                                          3004                                                                              S(CNH)NH.sub.2                                                                           1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)Ph                                                                         OH, OH                                          3005                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  H         (+)-pin                                         3006                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  Methyl    (+)-pin                                         3007                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  Ethyl     (+)-pin                                         3008                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl  (+)-pin                                         3009                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl   (+)-pin                                         3010                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         3011                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         3012                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         3013                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         3014                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         3015                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         3016                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                              (+)-pin                                         3017                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         3018                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         3019                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3  (+)-pin                                         3020                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                        (+)-pin                                         3021                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         3022                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         3023                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 Ph                                                                               (+)-pin                                         3024                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         3025                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         3026                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         3027                                                                              oMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         3028                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         3029                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         3030                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                        (+)-pin                                         3031                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         3032                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         3033                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                              (+)-pin                                         3034                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         3035                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         3036                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         3037                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         3038                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         3039                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 Ph                                                                            (+)-pin                                         3040                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 Ph                                                                            (+)-pin                                         3041                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 HPh                                                                           (+)-pin                                         3042                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 HPh                                                                           (+)-pin                                         3043                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 HPh                                                                           (+)-pin                                         3044                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 HPh                                                                           (+)-pin                                         3045                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         3046                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         3047                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  H         OH, OH                                          3048                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  Methyl    OH, OH                                          3049                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  Ethyl     OH, OH                                          3050                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl  OH, OH                                          3051                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl   OH, OH                                          3052                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                       OH, OH                                          3053                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          3054                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          3055                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          3056                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          3057                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          3058                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                              OH, OH                                          3059                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          3060                                                                              CMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          3061                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3  OH, OH                                          3062                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                        OH, OH                                          3063                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          3064                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          3065                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 Ph                                                                               OH, OH                                          3066                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          3067                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          3068                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          3069                                                                              oMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          3070                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          3071                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          3072                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                        OH, OH                                          3073                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          3074                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          3075                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                              OH, OH                                          3076                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                      OH, OH                                          3077                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                      OH, OH                                          3078                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          3079                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          3080                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          3081                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 Ph                                                                            OH, OH                                          3082                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 Ph                                                                            OH, OH                                          3083                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 HPh                                                                           OH, OH                                          3084                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 HPh                                                                           OH, OH                                          3085                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 HPh                                                                           OH, OH                                          3086                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 HPh                                                                           OH, OH                                          3087                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)Ph                                                                         OH, OH                                          3088                                                                              OMe       1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)Ph                                                                         OH, OH                                          3089                                                                              NH(CNH)H  1 Ph    H         (+)-pin                                         3090                                                                              NH(CNH)H  1 Ph    Methyl    (+)-pin                                         3091                                                                              NH(CNH)H  1 Ph    Ethyl     (+)-pin                                         3092                                                                              NH(CNH)H  1 Ph    n-Propyl  (+)-pin                                         3093                                                                              NH(CNH)H  1 Ph    n-Butyl   (+)-pin                                         3094                                                                              NH(CNH)H  1 Ph    CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         3095                                                                              NH(CNH)H  1 Ph    CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         3096                                                                              NH(CNH)H  1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         3097                                                                              NH(CNH)H  1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         3098                                                                              NH(CNH)H  1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         3099                                                                              NH(CNH)H  1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         3100                                                                              NH(CNH)H  1 Ph    CH.sub.2 CN                                                                              (+)-pin                                         3101                                                                              NH(CNH)H  1 Ph    CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         3102                                                                              NH(CNH)H  1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         3103                                                                              NH(CNH)H  1 Ph    CF.sub.3  (+)-pin                                         3104                                                                              NH(CNH)H  1 Ph    CF.sub.2 CF.sub.3                                                                        (+)-pin                                         3105                                                                              NH(CNH)H  1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         3106                                                                              NH(CNH)H  1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         3107                                                                              NH(CNH)H  1 Ph    F.sub.5 Ph                                                                               (+)-pin                                         3108                                                                              NH(CNH)H  1 Ph    CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         3109                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         3110                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         3111                                                                              NH(CNH)H  1 Ph    CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         3112                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         3113                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         3114                                                                              NH(CNH)H  1 Ph    CH.sub.2 NO.sub.2                                                                        (+)-pin                                         3115                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         3116                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         3117                                                                              NH(CNH)H  1 Ph    CH.sub.2 OH                                                                              (+)-pin                                         3118                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         3119                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         3120                                                                              NH(CNH)H  1 Ph    CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         3121                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         3122                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         3123                                                                              NH(CNH)H  1 Ph    3-NO.sub.2 Ph                                                                            (+)-pin                                         3124                                                                              NH(CNH)H  1 Ph    4-NO.sub.2 Ph                                                                            (+)-pin                                         3125                                                                              NH(CNH)H  1 Ph    3-CO.sub.2 HPh                                                                           (+)-pin                                         3126                                                                              NH(CNH)H  1 Ph    4-CO.sub.2 HPh                                                                           (+)-pin                                         3127                                                                              NH(CNH)H  1 Ph    3-CN.sub.4 HPh                                                                           (+)-pin                                         3128                                                                              NH(CNH)H  1 Ph    4-CN.sub.4 HPh                                                                           (+)-pin                                         3129                                                                              NH(CNH)H  1 Ph    3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         3130                                                                              NH(CNH)H  1 Ph    4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         3131                                                                              NH(CNH)H  1 Ph    H         OH, OH                                          3132                                                                              NH(CNH)H  1 Ph    Methyl    OH, OH                                          3133                                                                              NH(CNH)H  1 Ph    Ethyl     OH, OH                                          3134                                                                              NH(CNH)H  1 Ph    n-Propyl  OH, OH                                          3135                                                                              NH(CNH)H  1 Ph    n-Butyl   OH, OH                                          3136                                                                              NH(CNH)H  1 Ph    CH.sub.2 SCH.sub.3                                                                       OH, OH                                          3137                                                                              NH(CNH)H  1 Ph    CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          3138                                                                              NH(CNH)H  1 Ph    CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          3139                                                                              NH(CNH)H  1 Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          3140                                                                              NH(CNH)H  1 Ph    CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          3141                                                                              NH(CNH)H  1 Ph    CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          3142                                                                              NH(CNH)H  1 Ph    CH.sub.2 CN                                                                              OH, OH                                          3143                                                                              NH(CNH)H  1 Ph    CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          3144                                                                              NH(CNH)H  1 Ph    CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          3145                                                                              NH(CNH)H  1 Ph    CF.sub.3  OH, OH                                          3146                                                                              NH(CNH)H  1 Ph    CF.sub.2 CF.sub.3                                                                        OH, OH                                          3147                                                                              NH(CNH)H  1 Ph    CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          3148                                                                              NH(CNH)H  1 Ph    CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          3149                                                                              NH(CNH)H  1 Ph    F.sub.5 Ph                                                                               OH, OH                                          3150                                                                              NH(CNH)H  1 Ph    CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          3151                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          3152                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          3153                                                                              NH(CNH)H  1 Ph    CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          3154                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          3155                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          3156                                                                              NH(CNH)H  1 Ph    CH.sub.2 NO.sub.2                                                                        OH, OH                                          3157                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          3158                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          3159                                                                              NH(CNH)H  1 Ph    CH.sub.2 OH                                                                              OH, OH                                          3160                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.2 OH                                                                      OH, OH                                          3161                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.3 OH                                                                      OH, OH                                          3162                                                                              NH(CNH)H  1 Ph    CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          3163                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          3164                                                                              NH(CNH)H  1 Ph    (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          3165                                                                              NH(CNH)H  1 Ph    3-NO.sub.2 Ph                                                                            OH, OH                                          3166                                                                              NH(CNH)H  1 Ph    4-NO.sub.2 Ph                                                                            OH, OH                                          3167                                                                              NH(CNH)H  1 Ph    3-CO.sub.2 HPh                                                                           OH, OH                                          3168                                                                              NH(CNH)H  1 Ph    4-CO.sub.2 HPh                                                                           OH, OH                                          3169                                                                              NH(CNH)H  1 Ph    3-CN.sub.4 HPh                                                                           OH, OH                                          3170                                                                              NH(CNH)H  1 Ph    4-CN.sub.4 HPh                                                                           OH, OH                                          3171                                                                              NH(CNH)H  1 Ph    3-(HOCH.sub.2)Ph                                                                         OH, OH                                          3172                                                                              NH(CNH)H  1 Ph    4-(HOCH.sub.2)Ph                                                                         OH, OH                                          3173                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           H         (+)-pin                                         3174                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           Methyl    (+)-pin                                         3175                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           Ethyl     (+)-pin                                         3176                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           n-Propyl  (+)-pin                                         3177                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           n-Butyl   (+)-pin                                         3178                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         3179                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         3180                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         3181                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         3182                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         3183                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         3184                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                              (+)-pin                                         3185                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         3186                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         3187                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CF.sub.3  (+)-pin                                         3188                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                        (+)-pin                                         3189                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         3190                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         3191                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           F.sub.5 Ph                                                                               (+)-pin                                         3192                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         3193                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         3194                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         3195                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         3196                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         3197                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         3198                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                        (+)-pin                                         3199                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         3200                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         3201                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                              (+)-pin                                         3202                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         3203                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         3204                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         3205                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         3206                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         3207                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           3-NO.sub.2 Ph                                                                            (+)-pin                                         3208                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           4-NO.sub.2 Ph                                                                            (+)-pin                                         3209                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           3-CO.sub.2 HPh                                                                           (+)-pin                                         3210                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           4-CO.sub.2 HPh                                                                           (+)-pin                                         3211                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           3-CN.sub.4 HPh                                                                           (+)-pin                                         3212                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           4-CN.sub.4 HPh                                                                           (+)-pin                                         3213                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         3214                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         3215                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           H         OH, OH                                          3216                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           Methyl    OH, OH                                          3217                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           Ethyl     OH, OH                                          3218                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           n-Propyl  OH, OH                                          3219                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           n-Butyl   OH, OH                                          3220                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 SCH.sub.3                                                                       OH, OH                                          3221                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          3222                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          3223                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          3224                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          3225                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          3226                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CN                                                                              OH, OH                                          3227                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          3228                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          3229                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CF.sub.3  OH, OH                                          3230                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.3                                                                        OH, OH                                          3231                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          3232                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          3233                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           FSPh      OH, OH                                          3234                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          3235                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          3236                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          3237                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          3238                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          3239                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CN.sub.4 H                                                              OH,CH                                           3240                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 NO.sub.2                                                                        OH, OH                                          3241                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          3242                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          3243                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 OH                                                                              OH, OH                                          3244                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 OH                                                                      OH, OH                                          3245                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 OH                                                                      OH, OH                                          3246                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          3247                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          3248                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          3249                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           3-NO.sub.2 Ph                                                                            OH, OH                                          3250                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           4-NO.sub.2 Ph                                                                            OH, OH                                          3251                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           3-CO.sub.2 HPh                                                                           OH, OH                                          3252                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           4-CO.sub.2 HPh                                                                           OH, OH                                          3253                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           3-CN.sub.4 HPh                                                                           OH, OH                                          3254                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           4-CN.sub.4 HPh                                                                           OH, OH                                          3255                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           3-(HOCH.sub.2)Ph                                                                         OH, OH                                          3256                                                                              NH(CNH)H  1 PhCH.sub.2                                                                           4-(HOCH.sub.2)Ph                                                                         OH, OH                                          3257                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  H         (+)-pin                                         3258                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  Methyl    (+)-pin                                         3259                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  Ethyl     (+)-pin                                         3260                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl  (+)-pin                                         3261                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl   (+)-pin                                         3262                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                       (+)-pin                                         3263                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                    (+)-pin                                         3264                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                              (+)-pin                                         3265                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                              (+)-pin                                         3266                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           (+)-pin                                         3267                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    (+)-pin                                         3268                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                              (+)-pin                                         3269                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                     (+)-pin                                         3270                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            (+)-pin                                         3271                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3  (+)-pin                                         3272                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                        (+)-pin                                         3273                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                               (+)-pin                                         3274                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      (+)-pin                                         3275                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 Ph                                                                               (+)-pin                                         3276                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                      (+)-pin                                         3277                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                              (+)-pin                                         3278                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                              (+)-pin                                         3279                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                      (+)-pin                                         3280                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                              (+)-pin                                         3281                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                              (+)-pin                                         3282                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                        (+)-pin                                         3283                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                                (+)-pin                                         3284                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                                (+)-pin                                         3285                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                              (+)-pin                                         3286                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                      (+)-pin                                         3287                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                      (+)-pin                                         3288                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                     (+)-pin                                         3289                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                             (+)-pin                                         3290                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                             (+)-pin                                         3291                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 Ph                                                                            (+)-pin                                         3292                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 Ph                                                                            (+)-pin                                         3293                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 HPh                                                                           (+)-pin                                         3294                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 HPh                                                                           (+)-pin                                         3295                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 HPh                                                                           (+)-pin                                         3296                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 HPh                                                                           (+)-pin                                         3297                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)Ph                                                                         (+)-pin                                         3298                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)Ph                                                                         (+)-pin                                         3299                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  H         OH, OH                                          3300                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  Methyl    OH, OH                                          3301                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  Ethyl     OH, OH                                          3302                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  n-Propyl  OH, OH                                          3303                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  n-Butyl   OH, OH                                          3304                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 SCH.sub.3                                                                       OH, OH                                          3305                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO)CH.sub.3                                                                    OH, OH                                          3306                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 (SO.sub.2)CH.sub.3                                                              OH, OH                                          3307                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 SCH.sub.3                                                              OH, OH                                          3308                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO)CH.sub.3                                                           OH, OH                                          3309                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 (SO).sub.2 CH.sub.3                                                    OH, OH                                          3310                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN                                                                              OH, OH                                          3311                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CN                                                                     OH, OH                                          3312                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CH.sub.2 CH.sub.2 CN                                                            OH, OH                                          3313                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.3  OH, OH                                          3314                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.3                                                                        OH, OH                                          3315                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.3                                                               OH, OH                                          3316                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CF.sub.2 CF.sub.2 CF.sub.2 CF.sub.3                                                      OH, OH                                          3317                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  F.sub.5 Ph                                                                               OH, OH                                          3318                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 H                                                                      OH, OH                                          3319                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 H                                                              OH, OH                                          3320                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 H                                                              OH, OH                                          3321                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CN.sub.4 H                                                                      OH, OH                                          3322                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CN.sub.4 H                                                              OH, OH                                          3323                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CN.sub.4 H                                                              OH, OH                                          3324                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 NO.sub.2                                                                        OH, OH                                          3325                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 NO.sub.2                                                                OH, OH                                          3326                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 NO.sub.2                                                                OH, OH                                          3327                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 OH                                                                              OH, OH                                          3328                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 OH                                                                      OH, OH                                          3329                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 OH                                                                      OH, OH                                          3330                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  CH.sub.2 CO.sub.2 Me                                                                     OH, OH                                          3331                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.2 CO.sub.2 Me                                                             OH, OH                                          3332                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  (CH.sub.2).sub.3 CO.sub.2 Me                                                             OH, OH                                          3333                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  3-NO.sub.2 Ph                                                                            OH, OH                                          3334                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  4-NO.sub.2 Ph                                                                            OH, OH                                          3335                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  3-CO.sub.2 HPh                                                                           OH, OH                                          3336                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  4-CO.sub.2 HPh                                                                           OH, OH                                          3337                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  3-CN.sub.4 HPh                                                                           OH, OH                                          3338                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  4-CN.sub.4 HPh                                                                           OH, OH                                          3339                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  3-(HOCH.sub.2)Ph                                                                         OH, OH                                          3340                                                                              NH(CNH)H  1 PhCH.sub.2 CH.sub.2                                                                  4-(HOCH.sub.2)Ph                                                                         OH, OH                                          __________________________________________________________________________      BA. MS (M+H).sup.+ : Calc. 480, Found 480.                                     BC. MS (M+H).sup.+ : Calc. 494, Found 494.                                     BD. MS (M+H).sup.+ : Calc. 522, Found 522.                                     BE. MS (M+H).sup.+ : Calc. 540, Found 540.                                     BF. MS (M+H).sup.+ : Calc. 519, Found 519.                                     BG. MS (M+H).sup.+ : Calc. 538, Found 538.                                     BH. MS (M+H).sup.+ : Calc. 346, Found 346.                                     BI. MS (M+H).sup.+ : Calc. 494, Found 494.                                     BJ. Anal. calcd. for C.sub.17 H.sub.26 BN.sub.5 O.sub.3.2H.sub.2 O.1.8HCl      C, 44.30; H, 6.95; Cl, 13.84; N, 15.20. Found: C, 44.22; H, 6.66; Cl,          14.03; N, 14.03.                                                               BW. MS (M+H).sup.+ : Calc. 466, Found 466.                                     BX. MS (M+H).sup.+ : Calc. 480, Found 480.                                     CV. MS (M+H).sup.+ : Calc. 510, Found 510.                                     CW. MS (M+H).sup.+ : Calc. 600, Found 600.                                     CX. MS (M+H).sup.+ : Calc. 552, Found 552.                                     CY. MS (M+H).sup.+ : Calc. 629, Found 629.                                     CZ. MS (M+H).sup.+ : Calc. 524, Found 524.                                     DA. MS (M+H).sup.+ : Calc. 614, Found 614.                               

                  TABLE 16                                                         ______________________________________                                          ##STR111##                                                                                                                Phys.                              Ex   X            m     R.sup.13                                                                              R.sup.14                                                                              Y.sup.1 Y.sup.2                                                                      Data                               ______________________________________                                         3345 CH.sub.2 NH.sub.2                                                                           1     Ph     Ph     (+)-pin                                  3346 CH.sub.2 NH.sub.2                                                                           1     Ph     PhCH.sub.2                                                                            (+)-pin                                  3347 CH.sub.2 NH.sub.2                                                                           1     Ph     Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3348 CH.sub.2 NH.sub.2                                                                           1     PhCH.sub.2                                                                            Ph     (+)-pin                                  3349 CH.sub.2 NH.sub.2                                                                           1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            (+)-pin                                                                               BY                                3350 CH.sub.2 NH.sub.2                                                                           1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3351 CH.sub.2 NH.sub.2                                                                           1     Ph(CH.sub.2).sub.2                                                                    Ph     (+)-pin                                  3352 CH.sub.2 NH.sub.2                                                                           1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            (+)-pin                                  3353 CH.sub.2 NH.sub.2                                                                           1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3354 CH.sub.2 NH.sub.2                                                                           1     Ph     Ph     OH, OH                                   3355 CH.sub.2 NH.sub.2                                                                           1     Ph     PhCH.sub.2                                                                            OH, OH                                   3356 CH.sub.2 NH.sub.2                                                                           1     Ph     Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3357 CH.sub.2 NH.sub.2                                                                           1     PhCH.sub.2                                                                            Ph     OH, OH                                   3358 CH.sub.2 NH.sub.2                                                                           1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            OH, OH                                   3359 CH.sub.2 NH.sub.2                                                                           1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3360 CH.sub.2 NH.sub.2                                                                           1     Ph(CH.sub.2).sub.2                                                                    Ph     OH, OH                                   3361 CH.sub.2 NH.sub.2                                                                           1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            OH, OH                                   3362 CH.sub.2 NH.sub.2                                                                           1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3363 NH(CNH)NH.sub.2                                                                             1     Ph     Ph     (+)-pin                                  3364 NH(CNH)NH.sub.2                                                                             1     Ph     PhCH.sub.2                                                                            (+)-pin                                  3365 NH(CNH)NH.sub.2                                                                             1     Ph     Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3366 NH(CNH)NH.sub.2                                                                             1     PhCH.sub.2                                                                            Ph     (+)-pin                                  3367 NH(CNH)NH.sub.2                                                                             1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            (+)-pin                                  3368 NH(CNH)NH.sub.2                                                                             1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3369 NH(CNH)NH.sub.2                                                                             1     Ph(CH.sub.2).sub.2                                                                    Ph     (+)-pin                                  3370 NH(CNH)NH.sub.2                                                                             1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            (+)-pin                                  3371 NH(CNH)NH.sub.2                                                                             1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3372 NH(CNH)NH.sub.2                                                                             1     Ph     Ph     OH, OH                                   3373 NH(CNH)NH.sub.2                                                                             1     Ph     PhCH.sub.2                                                                            OH, OH                                   3374 NH(CNH)NH.sub.2                                                                             1     Ph     Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3375 NH(CNH)NH.sub.2                                                                             1     PhCH.sub.2                                                                            Ph     OH, OH                                   3376 NH(CNH)NH.sub.2                                                                             1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            OH, OH                                   3377 NH(CNH)NH.sub.2                                                                             1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3378 NH(CNH)NH.sub.2                                                                             1     Ph(CH.sub.2).sub.2                                                                    Ph     OH, OH                                   3379 NH(CNH)NH.sub.2                                                                             1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            OH, OH                                   3380 NH(CNH)NH.sub.2                                                                             1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3381 OMe          1     Ph     Ph     (+)-pin                                  3382 OMe          1     Ph     PhCH.sub.2                                                                            (+)-pin                                  3383 OMe          1     Ph     Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3384 OMe          1     PhCH.sub.2                                                                            Ph     (+)-pin                                  3385 OMe          1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            (+)-pin                                  3386 OMe          1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3387 OMe          1     Ph(CH.sub.2).sub.2                                                                    Ph     (+)-pin                                  3388 OMe          1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            (+)-pin                                  3389 OMe          1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3390 OMe          1     Ph     Ph     OH, OH                                   3391 OMe          1     Ph     PhCH.sub.2                                                                            OH, OH                                   3392 OMe          1     Ph     Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3393 OMe          1     PhCH.sub.2                                                                            Ph     OH, OH                                   3394 OMe          1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            OH, OH                                   3395 OMe          1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3396 OMe          1     Ph(CH.sub.2).sub.2                                                                    Ph     OH, OH                                   3397 OMe          1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            OH, OH                                   3398 OMe          1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3399 NH(CNH)H     1     Ph     Ph     (+)-pin                                  3400 NH(CNH)H     1     Ph     PhCH.sub.2                                                                            (+)-pin                                  3401 NH(CNH)H     1     Ph     Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3402 NH(CNH)H     1     PhCH.sub.2                                                                            Ph     (+)-pin                                  3403 NH(CNH)H     1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            (+)-pin                                  3404 NH(CNH)H     1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3405 NH(CNH)H     1     Ph(CH.sub.2).sub.2                                                                    Ph     (+)-pin                                  3406 NH(CNH)H     1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            (+)-pin                                  3407 NH(CNH)H     1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3408 NH(CNH)H     1     Ph     Ph     OH, OH                                   3409 NH(CNH)H     1     Ph     PhCH.sub.2                                                                            OH, OH                                   3410 NH(CNH)H     1     Ph     Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3411 NH(CNH)H     1     PhCH.sub.2                                                                            Ph     OH, OH                                   3412 NH(CNH)H     1     PhCH.sub.2                                                                            PhCH.sub.2                                                                            OH, OH                                   3413 NH(CNH)H     1     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3414 NH(CNH)H     1     Ph(CH.sub.2).sub.2                                                                    Ph     OH, OH                                   3415 NH(CNH)H     1     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            OH, OH                                   3416 NH(CNH)H     1     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3417 CH.sub.2 NH.sub.2                                                                           2     Ph     Ph     (+)-pin                                  3418 CH.sub.2 NH.sub.2                                                                           2     Ph     PhCH.sub.2                                                                            (+)-pin                                  3419 CH.sub.2 NH.sub.2                                                                           2     Ph     Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3420 CH.sub.2 NH.sub.2                                                                           2     PhCH.sub.2                                                                            Ph     (+)-pin                                  3421 CH.sub.2 NH.sub.2                                                                           2     PhCH.sub.2                                                                            PhCH.sub.2                                                                            (+)-pin                                  3422 CH.sub.2 NH.sub.2                                                                           2     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3423 CH.sub.2 NH.sub.2                                                                           2     Ph(CH.sub.2).sub.2                                                                    Ph     (+)-pin                                  3424 CH.sub.2 NH.sub.2                                                                           2     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            (+)-pin                                  3425 CH.sub.2 NH.sub.2                                                                           2     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3426 CH.sub.2 NH.sub.2                                                                           2     Ph     Ph     OH, OH                                   3427 CH.sub.2 NH.sub.2                                                                           2     Ph     PhCH.sub.2                                                                            OH, OH                                   3428 CH.sub.2 NH.sub.2                                                                           2     Ph     Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3429 CH.sub.2 NH.sub.2                                                                           2     PhCH.sub.2                                                                            Ph     OH, OH                                   3430 CH.sub.2 NH.sub.2                                                                           2     PhCH.sub.2                                                                            PhCH.sub.2                                                                            OH, OH                                   3431 CH.sub.2 NH.sub.2                                                                           2     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3432 CH.sub.2 NH.sub.2                                                                           2     Ph(CH.sub.2).sub.2                                                                    Ph     OH, OH                                   3433 CH.sub.2 NH.sub.2                                                                           2     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            OH, OH                                   3434 CH.sub.2 NH.sub.2                                                                           2     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3435 NH(CNH)NH.sub.2                                                                             2     Ph     Ph     (+)-pin                                  3436 NH(CNH)NH.sub.2                                                                             2     Ph     PhCH.sub.2                                                                            (+)-pin                                  3437 NH(CNH)NH.sub.2                                                                             2     Ph     Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3438 NH(CNH)NH.sub.2                                                                             2     PhCH.sub.2                                                                            Ph     (+)-pin                                  3439 NH(CNH)NH.sub.2                                                                             2     PhCH.sub.2                                                                            PhCH.sub.2                                                                            (+)-pin                                  3440 NH(CNH)NH.sub.2                                                                             2     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3441 NH(CNH)NH.sub.2                                                                             2     Ph(CH.sub.2).sub.2                                                                    Ph     (+)-pin                                  3442 NH(CNH)NH.sub.2                                                                             2     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            (+)-pin                                  3443 NH(CNH)NH.sub.2                                                                             2     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    (+)-pin                                  3444 NH(CNH)NH.sub.2                                                                             2     Ph     Ph     OH, OH                                   3445 NH(CNH)NH.sub.2                                                                             2     Ph     PhCH.sub.2                                                                            OH, OH                                   3446 NH(CNH)NH.sub.2                                                                             2     Ph     Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3447 NH(CNH)NH.sub.2                                                                             2     PhCH.sub.2                                                                            Ph     OH, OH                                   3448 NH(CNH)NH.sub.2                                                                             2     PhCH.sub.2                                                                            PhCH.sub.2                                                                            OH, OH                                   3449 NH(CNH)NH.sub.2                                                                             2     PhCH.sub.2                                                                            Ph(CH.sub.2).sub.2                                                                    OH, OH                                   3450 NH(CNH)NH.sub.2                                                                             2     Ph(CH.sub.2).sub.2                                                                    Ph     OH, OH                                   3451 NH(CNH)NH.sub.2                                                                             2     Ph(CH.sub.2).sub.2                                                                    PhCH.sub.2                                                                            OH, OH                                   3452 NH(CNH)NH.sub.2                                                                             2     Ph(CH.sub.2).sub.2                                                                    Ph(CH.sub.2).sub.2                                                                    OH, OH                                   ______________________________________                                          BY. MS (M+H)+: Calc. 570, Found 570.                                     

                                      TABLE 17                                     __________________________________________________________________________      ##STR112##                                                                                                         Phys.                                     Ex X        R.sup.13                                                                             R.sup.14  R.sup.15                                                                           Y.sup.1 Y.sup.2                                                                     Data                                      __________________________________________________________________________     3457                                                                              CH.sub.2 NH.sub.2                                                                       Ph    H         H   (+)-pin                                        3458                                                                              CH.sub.2 NH.sub.2                                                                       Ph    methyl    H   (+)-pin                                                                             BK                                        3459                                                                              CH.sub.2 NH.sub.2                                                                       Ph    methyl    H   (+)-pin                                        3460                                                                              CH.sub.2 NH.sub.2                                                                       Ph    methyl    methyl                                                                             (+)-pin                                        3461                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     H   (+)-pin                                        3462                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     methyl                                                                             (+)-pin                                        3463                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     ethyl                                                                              (+)-pin                                        3464                                                                              CH.sub.2 NH.sub.2                                                                       Ph    isopropyl H   (+)-pin                                        3465                                                                              CH.sub.2 NH.sub.2                                                                       Ph    phenyl    H   (+)-pin                                                                             BL                                        3466                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CN                                                                              H   (+)-pin                                        3467                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NC                                                                              H   (+)-pin                                        3468                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NO.sub.2                                                                        H   (+)-pin                                        3469                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SCH.sub.3                                                                       H   (+)-pin                                        3470                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SOCH.sub.3                                                                      H   (+)-pin                                        3471                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SO.sub.2 CH.sub.3                                                               H   (+)-pin                                        3472                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 OH                                                                              H   (+)-pin                                        3473                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 COOH                                                                            H   (+)-pin                                        3474                                                                              CH.sub.2 NH.sub.2                                                                       Ph    (CH.sub.2).sub.2 COOH                                                                    H   (+)-pin                                        3475                                                                              CH.sub.2 NH.sub.2                                                                       Ph    (CH.sub.2).sub.2 CN                                                                      H   (+)-pin                                        3476                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CHCHCOOMe H   (+)-pin                                        3477                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CHCHCOOH  H   (+)-pin                                        3478                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CHCHCN    H   (+)-pin                                        3479                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CN.sub.4 H                                                                      H   (+)-pin                                        3480                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NHSO.sub.2 CF.sub.3                                                             H   (+)-pin                                        3481                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 CN                                                                     H   (+)-pin                                        3482                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NC                                                                     H   (+)-pin                                        3483                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NO.sub.2                                                               H   (+)-pin                                        3484                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              H   (+)-pin                                        3485                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SOCH.sub.3                                                             H   (+)-pin                                        3486                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                      H   (+)-pin                                        3487                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 OH                                                                     H   (+)-pin                                        3488                                                                              CH.sub.2 NH.sub.2                                                                       Ph    NO.sub.2  H   (+)-pin                                        3489                                                                              CH.sub.2 NH.sub.2                                                                       Ph    F         H   (+)-pin                                        3490                                                                              CH.sub.2 NH.sub.2                                                                       Ph    OH        H   (+)-pin                                        3491                                                                              CH.sub.2 NH.sub.2                                                                       Ph    H         H   OH, OH                                         3492                                                                              CH.sub.2 NH.sub.2                                                                       Ph    methyl    H   OH, OH                                         3493                                                                              CH.sub.2 NH.sub.2                                                                       Ph    methyl    methyl                                                                             OH, OH                                         3494                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     H   OH, OH                                         3495                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     methyl                                                                             OH, OH                                         3496                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     ethyl                                                                              OH, OH                                         3497                                                                              CH.sub.2 NH.sub.2                                                                       Ph    isopropyl H   OH, OH                                         3498                                                                              CH.sub.2 NH.sub.2                                                                       Ph    phenyl    H   OH, OH                                         3499                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CN                                                                              H   OH, OH                                         3500                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NC                                                                              H   OH, OH                                         3501                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NO.sub.2                                                                        H   OH, OH                                         3502                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SCH.sub.2                                                                       H   OH, OH                                         3503                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SOCH.sub.3                                                                      H   OH, OH                                         3504                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SO.sub.2 CH.sub.3                                                               H   OH, OH                                         3505                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 OH                                                                              H   OH, OH                                         3506                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 COOH                                                                            H   OH, OH                                         3507                                                                              CH.sub.2 NH.sub.2                                                                       Ph    (CH.sub.2).sub.2 COOH                                                                    H   OH, OH                                         3508                                                                              CH.sub.2 NH.sub.2                                                                       Ph    (CH.sub.2).sub.2 CN                                                                      H   OH, OH                                         3509                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CHCHCOOMe H   OH, OH                                         3510                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CHCHCOOH  H   OH, OH                                         3511                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CN.sub.4 H                                                                      H   OH, OH                                         3512                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NHSO.sub.2 CF.sub.3                                                             H   OH, OH                                         3513                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 CN                                                                     H   OH, OH                                         3514                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NC                                                                     H   OH, OH                                         3515                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NO.sub.2                                                               H   OH, OH                                         3516                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              H   OH, OH                                         3517                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SOCH.sub.3                                                             H   OH, OH                                         3518                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                      H   OH, OH                                         3519                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 OH                                                                     H   OH, OH                                         3520                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 COOH                                                                   H   OH, OH                                         3521                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 CN.sub.4 H                                                             H   OH, OH                                         3522                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3                                                    H   OH, OH                                         3523                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                           H         H   (+)-pin                                        3524                                                                              CH.sub.2 NH.sub.2                                                                       PhO   methyl    H   (+)-pin                                        3525                                                                              CH.sub.2 NH.sub.2                                                                       PhS   methyl    methyl                                                                             (+)-pin                                        3526                                                                              CH.sub.2 NH.sub.2                                                                       PhNH  ethyl     H   (+)-pin                                        3527                                                                              CH.sub.2 NH.sub.2                                                                       PhCONH                                                                               ethyl     methyl                                                                             (+)-pin                                        3528                                                                              CH.sub.2 NH.sub.2                                                                       PhNHCO                                                                               ethyl     ethyl                                                                              (+)-pin                                        3529                                                                              CH.sub.2 NH.sub.2                                                                       Ph    isopropyl H   (+)-pin                                        3530                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                           phenyl    H   (+)-pin                                        3531                                                                              CH.sub.2 NH.sub.2                                                                       PhO   CH.sub.2 CN                                                                              H   (+)-pin                                        3532                                                                              CH.sub.2 NH.sub.2                                                                       PhS   CH.sub.2 NC                                                                              H   (+)-pin                                        3533                                                                              CH.sub.2 NH.sub.2                                                                       PhNH  CH.sub.2 NO.sub.2                                                                        H   (+)-pin                                        3534                                                                              CH.sub.2 NH.sub.2                                                                       PhCONH                                                                               CH.sub.2 SCH.sub.3                                                                       H   (+)-pin                                        3535                                                                              CH.sub.2 NH.sub.2                                                                       PhNHCO                                                                               CH.sub.2 SOCH.sub.3                                                                      H   (+)-pin                                        3536                                                                              CH.sub.2 NH.sub.2                                                                       Ph(CH.sub.2).sub.2                                                                   CH.sub.2 SO.sub.2 CH.sub.3                                                               H   (+)-pin                                        3537                                                                              NH(CNH)NH.sub.2                                                                         Ph    H         H   (+)-pin                                        3538                                                                              NH(CNH)NH.sub.2                                                                         Ph    methyl    H   (+)-pin                                                                             BM                                        3539                                                                              NH(CNH)NH.sub.2                                                                         Ph    methyl    H   (+)-pin                                        3540                                                                              NH(CNH)NH.sub.2                                                                         Ph    methyl    methyl                                                                             (+)-pin                                        3541                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     H   (+)-pin                                        3542                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     methyl                                                                             (+)-pin                                        3543                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     ethyl                                                                              (+)-pin                                        3544                                                                              NH(CNH)NH.sub.2                                                                         Ph    isopropyl H   (+)-pin                                        3545                                                                              NH(CNH)NH.sub.2                                                                         Ph    phenyl    H   (+)-pin                                        3546                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CN                                                                              H   (+)-pin                                        3547                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NC                                                                              H   (+)-pin                                        3548                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NO.sub.2                                                                        H   (+)-pin                                        3549                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SCH.sub.3                                                                       H   (+)-pin                                        3550                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SOCH.sub.3                                                                      H   (+)-pin                                        3551                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SO.sub.2 CH.sub.3                                                               H   (+)-pin                                        3552                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 OH                                                                              H   (+)-pin                                        3553                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 COOH                                                                            H   (+)-pin                                        3554                                                                              NH(CNH)NH.sub.2                                                                         Ph    (CH.sub.2).sub.2 COOH                                                                    H   (+)-pin                                        3555                                                                              NH(CNH)NH.sub.2                                                                         Ph    (CH.sub.2).sub.2 CN                                                                      H   (+)-pin                                        3556                                                                              NH(CNH)NH.sub.2                                                                         Ph    CHCHCOOMe H   (+)-pin                                        3557                                                                              NH(CNH)NH.sub.2                                                                         Ph    CHCHCOOH  H   (+)-pin                                        3558                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CN.sub.4 H                                                                      H   (+)-pin                                        3559                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NHSO.sub.2 CF.sub.3                                                             H   (+)-pin                                        3560                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 CN                                                                     H   (+)-pin                                        3561                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NC                                                                     H   (+)-pin                                        3562                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NO.sub.2                                                               H   (+)-pin                                        3563                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              H   (+)-pin                                        3564                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SOCH.sub.3                                                             H   (+)-pin                                        3565                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                      H   (+)-pin                                        3566                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 OH                                                                     H   (+)-pin                                        3567                                                                              NH(CNH)NH.sub.2                                                                         Ph    NO.sub.2  H   (+)-pin                                        3568                                                                              NH(CNH)NH.sub.2                                                                         Ph    F         H   (+)-pin                                        3569                                                                              NH(CNH)NH.sub.2                                                                         Ph    OH        H   (+)-pin                                        3570                                                                              NH(CNH)NH.sub.2                                                                         Ph    H         H   OH, OH                                         3571                                                                              NH(CNH)NH.sub.2                                                                         Ph    methyl    H   OH, OH                                         3572                                                                              NH(CNH)NH.sub.2                                                                         Ph    methyl    methyl                                                                             OH, OH                                         3573                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     H   OH, OH                                         3574                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     methyl                                                                             OH, OH                                         3575                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     ethyl                                                                              OH, OH                                         3576                                                                              NH(CNH)NH.sub.2                                                                         Ph    isopropyl H   OH, OH                                         3577                                                                              NH(CNH)NH.sub.2                                                                         Ph    phenyl    H   OH, OH                                         3578                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CN                                                                              H   OH, OH                                         3579                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NC                                                                              H   OH, OH                                         3580                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NO.sub.2                                                                        H   OH, OH                                         3581                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SCH.sub.3                                                                       H   OH, OH                                         3582                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SOCH.sub.3                                                                      H   OH, OH                                         3583                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SO.sub.2 CH.sub.3                                                               H   OH, OH                                         3584                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 OH                                                                              H   OH, OH                                         3585                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 COOH                                                                            H   OH, OH                                         3586                                                                              NH(CNH)NH.sub.2                                                                         Ph    (CH.sub.2).sub.2 COOH                                                                    H   OH, OH                                         3587                                                                              NH(CNH)NH.sub.2                                                                         Ph    (CH.sub.2).sub.2 CN                                                                      H   OH, OH                                         3588                                                                              NH(CNH)NH.sub.2                                                                         Ph    CHCHCOOMe H   OH, OH                                         3589                                                                              NH(CNH)NH.sub.2                                                                         Ph    CHCHCOOH  H   OH, OH                                         3590                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CN.sub.4 H                                                                      H   OH, OH                                         3591                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NHSO.sub.2 CF.sub.3                                                             H   OH, OH                                         3592                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 CN                                                                     H   OH, OH                                         3593                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NC                                                                     H   OH, OH                                         3594                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NO.sub.2                                                               H   OH, CH                                         3595                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              H   OH, OH                                         3596                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SOCH.sub.3                                                             H   OH, OH                                         3597                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                      H   OH, OH                                         3598                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 OH                                                                     H   OH, OH                                         3599                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 COOH                                                                   H   OH, OH                                         3600                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 CN.sub.4 H                                                             H   OH, OH                                         3601                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3                                                    H   OH, OH                                         3602                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                           H         H   (+)-pin                                        3603                                                                              NH(CNH)NH.sub.2                                                                         PhO   methyl    H   (+)-pin                                        3604                                                                              NH(CNH)NH.sub.2                                                                         PhS   methyl    methyl                                                                             (+)-pin                                        3605                                                                              NH(CNH)NH.sub.2                                                                         PhNH  ethyl     H   (+)-pin                                        3606                                                                              NH(CNH)NH.sub.2                                                                         PhCONH                                                                               ethyl     methyl                                                                             (+)-pin                                        3607                                                                              NH(CNH)NH.sub.2                                                                         PhNHCO                                                                               ethyl     ethyl                                                                              (+)-pin                                        3608                                                                              NH(CNH)NH.sub.2                                                                         Ph    isopropyl H   (+)-pin                                        3609                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                           phenyl    H   (+)-pin                                        3610                                                                              NH(CNH)NH.sub.2                                                                         PhO   CH.sub.2 CN                                                                              H   (+)-pin                                        3611                                                                              NH(CNH)NH.sub.2                                                                         PhS   CH.sub.2 NC                                                                              H   (+)-pin                                        3612                                                                              NH(CNH)NH.sub.2                                                                         PhNH  CH.sub.2 NO.sub.2                                                                        H   (+)-pin                                        3613                                                                              NH(CNH)NH.sub.2                                                                         PhCONH                                                                               CH.sub.2 SCH.sub.3                                                                       H   (+)-pin                                        3614                                                                              NH(CNH)NH.sub.2                                                                         PhNHCO                                                                               CH.sub.2 SOCH.sub.3                                                                      H   (+)-pin                                        3615                                                                              NH(CNH)NH.sub.2                                                                         Ph(CH.sub.2).sub.2                                                                   CH.sub.2 SO.sub.2 CH.sub.3                                                               H   (+)-pin                                        3616                                                                              OMe      Ph    CH.sub.3  H   (+)-pin                                        3617                                                                              NH(CNH)H Ph    CH.sub.3  H   (+)-pin                                        3618                                                                              OMe      Ph    CH.sub.3  H   OH, OH                                         3619                                                                              NH(CNH)H Ph    CH.sub.3  H   OH, OH                                         __________________________________________________________________________      BK. MS (MH).sup.+ : Calc. 477, Found 477.                                      BL. MS (MH).sup.+ : Calc. 539, Found 539.                                      BM. MS (MH).sup.+ : Calc. 505, Found 505.                                

                                      TABLE 18                                     __________________________________________________________________________      ##STR113##                                                                                                         Phys.                                     Ex X        R.sup.13                                                                             R.sup.14  R.sup.15                                                                           Y.sup.1 Y.sup.2                                                                     Data                                      __________________________________________________________________________     3624                                                                              CH.sub.2 NH.sub.2                                                                       Ph    H         H   (+)-pin                                        3625                                                                              CH.sub.2 NH.sub.2                                                                       Ph    methyl    H   (+)-pin                                        3626                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     H   (+)-pin                                        3627                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     methyl                                                                             (+)-pin                                        3628                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     ethyl                                                                              (+)-pin                                        3629                                                                              CH.sub.2 NH.sub.2                                                                       Ph    isopropyl H   (+)-pin                                        3630                                                                              CH.sub.2 NH.sub.2                                                                       Ph    phenyl    H   (+)-pin                                        3631                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CN                                                                              H   (+)-pin                                        3632                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NC                                                                              H   (+)-pin                                        3633                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NO.sub.2                                                                        H   (+)-pin                                        3634                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SCH.sub.3                                                                       H   (+)-pin                                        3635                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SOCH.sub.3                                                                      H   (+)-pin                                        3636                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SO.sub.2 CH.sub.3                                                               H   (+)-pin                                        3637                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 OH                                                                              H   (+)-pin                                        3638                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 COOH                                                                            H   (+)-pin                                        3639                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CN.sub.4 H                                                                      H   (+)-pin                                        3640                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NHSO.sub.2 CF.sub.3                                                             H   (+)-pin                                        3641                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 CN                                                                     H   (+)-pin                                        3642                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NC                                                                     H   (+)-pin                                        3643                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NO.sub.2                                                               H   (+)-pin                                        3644                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              H   (+)-pin                                        3645                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SOCH.sub.3                                                             H   (+)-pin                                        3646                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                      H   (+)-pin                                        3647                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 OH                                                                     H   (+)-pin                                        3648                                                                              CH.sub.2 NH.sub.2                                                                       Ph    NO.sub.2  H   (+)-pin                                        3649                                                                              CH.sub.2 NH.sub.2                                                                       Ph    F         H   (+)-pin                                        3650                                                                              CH.sub.2 NH.sub.2                                                                       Ph    OH        H   (+)-pin                                        3651                                                                              CH.sub.2 NH.sub.2                                                                       Ph    H         H   OH, OH                                         3652                                                                              CH.sub.2 NH.sub.2                                                                       Ph    methyl    H   OH, OH                                         3653                                                                              CH.sub.2 NH.sub.2                                                                       Ph    methyl    methyl                                                                             OH, CH                                         3654                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     H   OH, OH                                         3655                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     methyl                                                                             OH, OH                                         3656                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     ethyl                                                                              OH, OH                                         3657                                                                              CH.sub.2 NH.sub.2                                                                       Ph    isopropyl H   OH, OH                                         3658                                                                              CH.sub.2 NH.sub.2                                                                       Ph    phenyl    H   OH, OH                                         3659                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CN                                                                              H   OH, OH                                         3660                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NC                                                                              H   OH, OH                                         3661                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NO.sub.2                                                                        H   OH, OH                                         3662                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SCH.sub.3                                                                       H   OH, OH                                         3663                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SOCH.sub.3                                                                      H   OH, OH                                         3664                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SO.sub.2 CH.sub.3                                                               H   OH, OH                                         3665                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 OH                                                                              H   OH, OH                                         3666                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 COOH                                                                            H   OH, OH                                         3667                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CN.sub.4 H                                                                      H   OH, OH                                         3668                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NHSO.sub.2 CF.sub.3                                                             H   OH, OH                                         3669                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 CN                                                                     H   OH, OH                                         3670                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NC                                                                     H   OH, OH                                         3671                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NO.sub.2                                                               H   OH, OH                                         3672                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              H   OH, Off                                        3673                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SOCH.sub.3                                                             H   OH, OH                                         3674                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                      H   OH, OH                                         3675                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 OH                                                                     H   OH, OH                                         3676                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 COOH                                                                   H   OH, OH                                         3677                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 CN.sub.4 H                                                             H   OH, OH                                         3678                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3                                                    H   OH, OH                                         3679                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                           H         H   (+)-pin                                        3680                                                                              CH.sub.2 NH.sub.2                                                                       PhO   methyl    H   (+)-pin                                        3681                                                                              CH.sub.2 NH.sub.2                                                                       PhS   methyl    methyl                                                                             (+)-pin                                        3682                                                                              CH.sub.2 NH.sub.2                                                                       PhNH  ethyl     H   (+)-pin                                        3683                                                                              CH.sub.2 NH.sub.2                                                                       PhCONH                                                                               ethyl     methyl                                                                             (+)-pin                                        3684                                                                              CH.sub.2 NH.sub.2                                                                       PhNHCO                                                                               ethyl     ethyl                                                                              (+)-pin                                        3685                                                                              CH.sub.2 NH.sub.2                                                                       Ph    isopropyl H   (+)-pin                                        3686                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                           phenyl    H   (+)-pin                                        3687                                                                              CH.sub.2 NH.sub.2                                                                       PhO   CH.sub.2 CN                                                                              H   (+)-pin                                        3688                                                                              CH.sub.2 NH.sub.2                                                                       PhS   CH.sub.2 NC                                                                              H   (+)-pin                                        3689                                                                              CH.sub.2 NH.sub.2                                                                       PhNH  CH.sub.2 NO.sub.2                                                                        H   (+)-pin                                        3690                                                                              CH.sub.2 NH.sub.2                                                                       PhCONH                                                                               CH.sub.2 SCH.sub.3                                                                       H   (+)-pin                                        3691                                                                              CH.sub.2 NH.sub.2                                                                       PhNHCO                                                                               CH.sub.2 SOCH.sub.3                                                                      H   (+)-pin                                        3692                                                                              CH.sub.2 NH.sub.2                                                                       Ph(CH.sub.2).sub.2                                                                   CH.sub.2 SO.sub.2 CH.sub.3                                                               H   (+)-pin                                        3693                                                                              NH(CNH)NH.sub.2                                                                         Ph    H         H   (+)-pin                                        3694                                                                              NH(CNH)NH.sub.2                                                                         Ph    methyl    methyl                                                                             (+)-pin                                        3695                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     H   (+)-pin                                        3696                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     methyl                                                                             (+)-pin                                        3697                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     ethyl                                                                              (+)-pin                                        3698                                                                              NH(CNH)NH.sub.2                                                                         Ph    isopropyl H   (+)-pin                                        3699                                                                              NH(CNH)NH.sub.2                                                                         Ph    phenyl    H   (+)-pin                                        3700                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CN                                                                              H   (+)-pin                                        3701                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NC                                                                              H   (+)-pin                                        3702                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NO.sub.2                                                                        H   (+)-pin                                        3703                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SCH.sub.3                                                                       H   (+)-pin                                        3704                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SOCH.sub.3                                                                      H   (+)-pin                                        3705                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SO.sub.2 CH.sub.3                                                               H   (+)-pin                                        3706                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 OH                                                                              H   (+)-pin                                        3707                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 COOH                                                                            H   (+)-pin                                        3708                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CN.sub.4 H                                                                      H   (+)-pin                                        3709                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NHSO.sub.2 CF.sub.3                                                             H   (+)-pin                                        3710                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 CN                                                                     H   (+)-pin                                        3711                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NC                                                                     H   (+)-pin                                        3712                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NO.sub.2                                                               H   (+)-pin                                        3713                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              H   (+)-pin                                        3714                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SOCH.sub.3                                                             H   (+)-pin                                        3715                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                      H   (+)-pin                                        3716                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 OH                                                                     H   (+)-pin                                        3717                                                                              NH(CNH)NH.sub.2                                                                         Ph    NO.sub.2  H   (+)-pin                                        3718                                                                              NH(CNH)NH.sub.2                                                                         Ph    F         H   (+)-pin                                        3719                                                                              NH(CNH)NH.sub.2                                                                         Ph    OH        H   (+)-pin                                        3720                                                                              NH(CNH)NH.sub.2                                                                         Ph    H         H   OH, OH                                         3721                                                                              NH(CNH)NH.sub.2                                                                         Ph    methyl    H   OH, OH                                         3722                                                                              NH(CNH)NH.sub.2                                                                         Ph    methyl    methyl                                                                             OH, OH                                         3723                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     H   OH, OH                                         3724                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     methyl                                                                             OH, OH                                         3725                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     ethyl                                                                              OH, OH                                         3726                                                                              NH(CNH)NH.sub.2                                                                         Ph    isopropyl H   OH, OH                                         3727                                                                              NH(CNH)NH.sub.2                                                                         Ph    phenyl    H   OH, OH                                         3728                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CN                                                                              H   OH, OH                                         3729                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NC                                                                              H   OH, OH                                         3730                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NO.sub.2                                                                        H   OH, OH                                         3731                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SCH.sub.3                                                                       H   OH, OH                                         3732                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SOCH.sub.3                                                                      H   OH, OH                                         3733                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SO.sub.2 CH.sub.3                                                               H   OH, OH                                         3734                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 OH                                                                              H   OH, OH                                         3735                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 COOH                                                                            H   OH, OH                                         3736                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CN.sub.4 H                                                                      H   OH, OH                                         3737                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NHSO.sub.2 CF.sub.3                                                             H   OH, OH                                         3738                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 CN                                                                     H   OH, OH                                         3739                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NC                                                                     H   OH, OH                                         3740                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NO.sub.2                                                               H   OH, OH                                         3741                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              H   OH, OH                                         3742                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SOCH.sub.3                                                             H   OH, OH                                         3743                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                      H   OH, OH                                         3744                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 OH                                                                     H   OH, OH                                         3745                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 COOH                                                                   B   OH, OH                                         3746                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 CN.sub.4 H                                                             H   OH, OH                                         3747                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3                                                    H   OH, OH                                         3748                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                           H         H   (+)-pin                                        3749                                                                              NH(CNH)NH.sub.2                                                                         PhO   methyl    H   (+)-pin                                        3750                                                                              NH(CNH)NH.sub.2                                                                         PhS   methyl    methyl                                                                             (+)-pin                                        3751                                                                              NH(CNH)NH.sub.2                                                                         PhNH  ethyl     H   (+)-pin                                        3752                                                                              NH(CNH)NH.sub.2                                                                         PhCONH                                                                               ethyl     methyl                                                                             (+)-pin                                        3753                                                                              NH(CNH)NH.sub.2                                                                         PhNHCO                                                                               ethyl     ethyl                                                                              (+)-pin                                        3754                                                                              NH(CNH)NH.sub.2                                                                         Ph    isopropyl H   (+)-pin                                        3755                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                           phenyl    H   (+)-pin                                        3756                                                                              NH(CNH)NH.sub.2                                                                         PhO   CH.sub.2 CN                                                                              H   (+)-pin                                        3757                                                                              NH(CNH)NH.sub.2                                                                         PhS   CH.sub.2 NC                                                                              H   (+)-pin                                        3758                                                                              NH(CNH)NH.sub.2                                                                         PhNH  CH.sub.2 NO.sub.2                                                                        H   (+)-pin                                        3759                                                                              NH(CNH)NH.sub.2                                                                         PhCONH                                                                               CH.sub.2 SCH.sub.3                                                                       H   (+)-pin                                        3760                                                                              NH(CNH)NH.sub.2                                                                         PhNHCO                                                                               CH.sub.2 SOCH.sub.3                                                                      H   (+)-pin                                        3761                                                                              NH(CNH)NH.sub.2                                                                         Ph(CH.sub.2).sub.2                                                                   CH.sub.2 SO.sub.2 CH.sub.3                                                               H   (+)-pin                                        3762                                                                              OMe      Ph    CH.sub.3  H   (+)-pin                                        3763                                                                              NH(CNH)H Ph    CH.sub.3  H   (+)-pin                                        3764                                                                              OMe      Ph    CH.sub.3  H   OH, OH                                         3765                                                                              NH(CNH)H Ph    CH.sub.3  H   OH, OH                                         __________________________________________________________________________

                  TABLE 19                                                         ______________________________________                                          ##STR114##                                                                                                               Phys.                               Ex   X            R.sup.13                                                                              R.sup.14                                                                             R.sup.15                                                                            Y.sup.1 Y.sup.2                                                                       Data                                ______________________________________                                         3770 CH.sub.2 NH.sub.2                                                                           Ph     H     H    (+)-pin                                    3771 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               H    (+)-pin                                    3772 CH.sub.2 NH.sub.2                                                                           Ph     H     H    OH, OH                                     3773 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               H    OH, OH                                     3774 NH(CNH)NH.sub.2                                                                             Ph     H     H    (+)-pin                                    3775 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               H    (+)-pin                                    3776 NH(CNH)NH.sub.2                                                                             Ph     H     H    OH, OH                                     3777 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               H    OH, OH                                     3778 OMe          Ph     CH.sub.3                                                                             H    (+)-pin                                    3779 NH(CNH)H     Ph     CH.sub.3                                                                             H    (+)-pin                                    3780 OMe          Ph     CH.sub.3                                                                             H    OH, OH                                     3781 NH(CNH)H     Ph     CH.sub.3                                                                             H    OH, OH                                     ______________________________________                                    

                                      TABLE 20                                     __________________________________________________________________________      ##STR115##                                                                                                         Phys.                                     Ex X        R.sup.13                                                                             R.sup.14  R.sup.15                                                                           Y.sup.1 Y.sup.2                                                                     Data                                      __________________________________________________________________________     3786                                                                              CH.sub.2 NH.sub.2                                                                       Ph    H         H   (+)-pin                                        3787                                                                              CH.sub.2 NH.sub.2                                                                       Ph    methyl    methyl                                                                             (+)-pin                                        3788                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     H   (+)-pin                                        3789                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     methyl                                                                             (+)-pin                                        3790                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     ethyl                                                                              (+)-pin                                        3791                                                                              CH.sub.2 NH.sub.2                                                                       Ph    isopropyl H   (+)-pin                                        3792                                                                              CH.sub.2 NH.sub.2                                                                       Ph    phenyl    H   (+)-pin                                        3793                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CN                                                                              H   (+)-pin                                        3794                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NC                                                                              H   (+)-pin                                        3795                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NO.sub.2                                                                        H   (+)-pin                                        3796                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SCH.sub.3                                                                       H   (+)-pin                                        3797                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SOCH.sub.3                                                                      H   (+)-pin                                        3798                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SO.sub.2 CH.sub.3                                                               H   (+)-pin                                        3799                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 OH                                                                              H   (+)-pin                                        3800                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 COOH                                                                            H   (+)-pin                                        3801                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CN.sub.4 H                                                                      H   (+)-pin                                        3802                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NHSO.sub.2 CF.sub.3                                                             H   (*)-pin                                        3803                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 CN                                                                     H   (+)-pin                                        3804                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NC                                                                     H   (+)-pin                                        3805                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NO.sub.2                                                               H   (+)-pin                                        3806                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              H   (+)-pin                                        3807                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SOCH.sub.3                                                             H   (+)-pin                                        3808                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                      H   (+)-pin                                        3809                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 OH                                                                     H   (+)-pin                                        3810                                                                              CH.sub.2 NH.sub.2                                                                       Ph    NO.sub.2  H   (+)-pin                                        3811                                                                              CH.sub.2 NH.sub.2                                                                       Ph    F         H   (+)-pin                                        3812                                                                              CH.sub.2 NH.sub.2                                                                       Ph    OH        H   (+)-pin                                        3813                                                                              CH.sub.2 NH.sub.2                                                                       Ph    H         H   OH, OH                                         3814                                                                              CH.sub.2 NH.sub.2                                                                       Ph    methyl    H   OH, OH                                         3815                                                                              CH.sub.2 NH.sub.2                                                                       Ph    methyl    methyl                                                                             OH, OH                                         3816                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     H   OH, OH                                         3817                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     methyl                                                                             OH, OH                                         3818                                                                              CH.sub.2 NH.sub.2                                                                       Ph    ethyl     ethyl                                                                              OH, OH                                         3819                                                                              CH.sub.2 NH.sub.2                                                                       Ph    isopropyl H   OH, OH                                         3820                                                                              CH.sub.2 NH.sub.2                                                                       Ph    phenyl    H   OH, OH                                         3821                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CN                                                                              H   OH, OH                                         3822                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NC                                                                              H   OH, OH                                         3823                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NO.sub.2                                                                        H   OH, OH                                         3824                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SCH.sub.3                                                                       H   OH, OH                                         3825                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SOCH.sub.3                                                                      H   OH, OH                                         3826                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 SO.sub.2 CH.sub.3                                                               H   OH, OH                                         3827                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 OH                                                                              H   OH, OH                                         3828                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 COOH                                                                            H   OH, OH                                         3829                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CN.sub.4 H                                                                      H   OH, OH                                         3830                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 NHSO.sub.2 CF.sub.3                                                             H   OH, OH                                         3831                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 CN                                                                     H   OH, OH                                         3832                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NC                                                                     H   OH, OH                                         3833                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NO.sub.2                                                               H   OH, OH                                         3834                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              H   OH, OH                                         3835                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SOCH.sub.3                                                             H   OH, OH                                         3836                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                      H   OH, OH                                         3837                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 OH                                                                     H   OH, OH                                         3838                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 COOH                                                                   H   OH, OH                                         3839                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 CN.sub.4 H                                                             H   OH, OH                                         3840                                                                              CH.sub.2 NH.sub.2                                                                       Ph    CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3                                                    H   OH, OH                                         3841                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                           H         H   (+)-pin                                        3842                                                                              CH.sub.2 NH.sub.2                                                                       PhO   methyl    H   (+)-pin                                        3843                                                                              CH.sub.2 NH.sub.2                                                                       PhS   methyl    methyl                                                                             (+)-pin                                        3844                                                                              CH.sub.2 NH.sub.2                                                                       PhNH  ethyl     H   (+)-pin                                        3845                                                                              CH.sub.2 NH.sub.2                                                                       PhCONH                                                                               ethyl     methyl                                                                             (+)-pin                                        3846                                                                              CH.sub.2 NH.sub.2                                                                       PhNHCO                                                                               ethyl     ethyl                                                                              (+)-pin                                        3847                                                                              CH.sub.2 NH.sub.2                                                                       Ph    isopropyl H   (+)-pin                                        3848                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                           phenyl    H   (+)-pin                                        3849                                                                              CH.sub.2 NH.sub.2                                                                       PhO   CH.sub.2 CN                                                                              H   (+)-pin                                        3850                                                                              CH.sub.2 NH.sub.2                                                                       PhS   CH.sub.2 NC                                                                              H   (+)-pin                                        3851                                                                              CH.sub.2 NH.sub.2                                                                       PhNH  CH.sub.2 NO.sub.2                                                                        H   (+)-pin                                        3852                                                                              CH.sub.2 NH.sub.2                                                                       PhCONH                                                                               CH.sub.2 SCH.sub.3                                                                       H   (+)-pin                                        3853                                                                              CH.sub.2 NH.sub.2                                                                       PhNHCO                                                                               CH.sub.2 SOCH.sub.3                                                                      H   (+)-pin                                        3854                                                                              CH.sub.2 NH.sub.2                                                                       Ph(CH.sub.2).sub.2                                                                   CH.sub.2 SO.sub.2 CH.sub.3                                                               H   (+)-pin                                        3855                                                                              NH(CNH)NH.sub.2                                                                         Ph    H         H   (+)-pin                                        3856                                                                              NH(CNH)NH.sub.2                                                                         Ph    methyl    methyl                                                                             (+)-pin                                        3857                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     H   (+)-pin                                        3858                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     methyl                                                                             (+)-pin                                        3859                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     ethyl                                                                              (+)-pin                                        3860                                                                              NH(CNH)NH.sub.2                                                                         Ph    isopropyl H   (+)-pin                                        3861                                                                              NH(CNH)NH.sub.2                                                                         Ph    phenyl    H   (+)-pin                                        3862                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CN                                                                              H   (+)-pin                                        3863                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NC                                                                              H   (+)-pin                                        3864                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NO.sub.2                                                                        H   (+)-pin                                        3865                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SCH.sub.3                                                                       H   (+)-pin                                        3866                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SOCH.sub.3                                                                      H   (+)-pin                                        3867                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SO.sub.2 CH.sub.3                                                               H   (+)-pin                                        3868                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 OH                                                                              H   (+)-pin                                        3869                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 COOH                                                                            H   (+)-pin                                        3870                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CN.sub.4 H                                                                      H   (+)-pin                                        3871                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NHSO.sub.2 CF.sub.3                                                             H   (+)-pin                                        3872                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 CN                                                                     H   (+)-pin                                        3873                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NC                                                                     H   (+)-pin                                        3874                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NO.sub.2                                                               H   (+)-pin                                        3875                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              H   (+)-pin                                        3876                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SOCH.sub.3                                                             H   (+)-pin                                        3877                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                      H   (+)-pin                                        3878                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 OH                                                                     H   (+)-pin                                        3879                                                                              NH(CNH)NH.sub.2                                                                         Ph    NO.sub.2  H   (+)-pin                                        3880                                                                              NH(CNH)NH.sub.2                                                                         Ph    F         H   (+)-pin                                        3881                                                                              NH(CNH)NH.sub.2                                                                         Ph    OH        H   (+)-pin                                        3882                                                                              NH(CNH)NH.sub.2                                                                         Ph    H         H   OH, OH                                         3883                                                                              NH(CNH)NH.sub.2                                                                         Ph    methyl    H   OH, OH                                         3884                                                                              NH(CNH)NH.sub.2                                                                         Ph    methyl    methyl                                                                             OH, OH                                         3885                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     H   OH, OH                                         3886                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     methyl                                                                             OH, OH                                         3887                                                                              NH(CNH)NH.sub.2                                                                         Ph    ethyl     ethyl                                                                              OH, OH                                         3888                                                                              NH(CNH)NH.sub.2                                                                         Ph    isopropyl H   OH, OH                                         3889                                                                              NH(CNH)NH.sub.2                                                                         Ph    phenyl    H   OH, OH                                         3890                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CN                                                                              H   OH, OH                                         3891                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NC                                                                              H   OH, OH                                         3892                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NO.sub.2                                                                        H   OH, OH                                         3893                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SCH.sub.3                                                                       H   OH, CF                                         3894                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SOCH.sub.3                                                                      H   OH, OH                                         3895                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 SO.sub.2 CH.sub.3                                                               H   OH, OH                                         3896                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 OH                                                                              H   OH, OH                                         3897                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 COOH                                                                            H   OH, OH                                         3898                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CN.sub.4 H                                                                      H   OH, OH                                         3899                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 NHSO.sub.2 CF.sub.3                                                             H   OH, OH                                         3900                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 CN                                                                     H   OH, OH                                         3901                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NC                                                                     H   OH, OH                                         3902                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NO.sub.2                                                               H   OH, OH                                         3903                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SCH.sub.3                                                              H   OH, OH                                         3904                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SOCH.sub.3                                                             H   OH, OH                                         3905                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.3                                                      H   OH, OH                                         3906                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 OH                                                                     H   OH, OH                                         3907                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 COOH                                                                   H   OH, OH                                         3908                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 CN.sub.4 H                                                             H   OH, OH                                         3909                                                                              NH(CNH)NH.sub.2                                                                         Ph    CH.sub.2 CH.sub.2 NHSO.sub.2 CF.sub.3                                                    H   OH, OH                                         3910                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                           H         H   (+)-pin                                        3911                                                                              NH(CNH)NH.sub.2                                                                         PhO   methyl    H   (+)-pin                                        3912                                                                              NH(CNH)NH.sub.2                                                                         PhS   methyl    methyl                                                                             (+)-pin                                        3913                                                                              NH(CNH)NH.sub.2                                                                         PhNH  ethyl     H   (+)-pin                                        3914                                                                              NH(CNH)NH.sub.2                                                                         PhCONH                                                                               ethyl     methyl                                                                             (+)-pin                                        3915                                                                              NH(CNH)NH.sub.2                                                                         PhNHCO                                                                               ethyl     ethyl                                                                              (+)-pin                                        3916                                                                              NH(CNH)NH.sub.2                                                                         Ph    isopropyl H   (+)-pin                                        3917                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                           phenyl    H   (+)-pin                                        3918                                                                              NH(CNH)NH.sub.2                                                                         PhO   CH.sub.2 CN                                                                              H   (+)-pin                                        3919                                                                              NH(CNH)NH.sub.2                                                                         PhS   CH.sub.2 NC                                                                              H   (+)-pin                                        3920                                                                              NH(CNH)NH.sub.2                                                                         PhNH  CH.sub.2 NO.sub.2                                                                        H   (+)-pin                                        3921                                                                              NH(CNH)NH.sub.2                                                                         PhCONH                                                                               CH.sub.2 SCH.sub.3                                                                       H   (+)-pin                                        3922                                                                              NH(CNH)NH.sub.2                                                                         PhNHCO                                                                               CH.sub.2 SOCH.sub.3                                                                      H   (+)-pin                                        3923                                                                              NH(CNH)NH.sub.2                                                                         Ph(CH.sub.2).sub.2                                                                   CH.sub.2 SO.sub.2 CH.sub.3                                                               H   (+)-pin                                        3924                                                                              OMe      Ph    CH.sub.3  H   (+)-pin                                        3925                                                                              NH(CNH)H Ph    CH.sub.3  H   (+)-pin                                        3926                                                                              OMe      Ph    CH.sub.3  H   OH, OH                                         3927                                                                              NH(CNH)H Ph    CH.sub.3  H   OH, OH                                         __________________________________________________________________________

                  TABLE 21                                                         ______________________________________                                          ##STR116##                                                                                                               Phys.                               Ex   X            R.sup.13                                                                              R.sup.14                                                                             R.sup.15                                                                            Y.sup.1 Y.sup.2                                                                       Data                                ______________________________________                                         3932 CH.sub.2 NH.sub.2                                                                           Ph     H     H    (+)-pin                                    3933 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               H    (+)-pin                                    3934 CH.sub.2 NH.sub.2                                                                           Ph     H     H    OH, OH                                     3935 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               H    OH, OH                                     3936 NH(CNH)NH.sub.2                                                                             Ph     H     H    (+)-pin                                    3937 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               H    (+)-pin                                    3938 NH(CNH)NH.sub.2                                                                             Ph     H     H    OH, OH                                     3939 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               H    OH, OH                                     3940 OMe          Ph     CH.sub.3                                                                             H    (+)-pin                                    3941 NH(CNH)H     Ph     CH.sub.3                                                                             H    (+)-pin                                    3942 OMe          Ph     CH.sub.3                                                                             H    OH, OH                                     3943 NH(CNH)H     Ph     CH.sub.3                                                                             H    OH, OH                                     ______________________________________                                    

                  TABLE 22                                                         ______________________________________                                          ##STR117##                                                                    Ex   X            R.sup.13                                                                              R.sup.14                                                                             Y.sup.1 Y.sup.2                                                                       Phys. Data                               ______________________________________                                         3948 CH.sub.2 NH.sub.2                                                                           Ph     H     (+)-pin                                         3949 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               (+)-pin                                         3950 CH.sub.2 NH.sub.2                                                                           Ph     H     OH, OH                                          3951 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               OH, OH                                          3952 NH(CNH)NH.sub.2                                                                             Ph     H     (+)-pin                                         3953 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               (+)-pin                                         3954 NH(CNH)NH.sub.2                                                                             Ph     H     OH, OH                                          3955 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               OH, OH                                          3956 OMe          Ph     CH.sub.3                                                                             (+)-pin                                         3957 NH(CNH)H     Ph     CH.sub.3                                                                             (+)-pin                                         3958 OMe          Ph     CH.sub.3                                                                             OH, OH                                          3959 NH(CNH)H     Ph     CH.sub.3                                                                             OH, OH                                          ______________________________________                                    

                  TABLE 23                                                         ______________________________________                                          ##STR118##                                                                    Ex   X            R.sup.13                                                                              R.sup.14                                                                             Y.sup.1 Y.sup.2                                                                       Phys. Data                               ______________________________________                                         3964 CH.sub.2 NH.sub.2                                                                           Ph     H     (+)-pin                                         3965 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               (+)-pin                                         3966 CH.sub.2 NH.sub.2                                                                           Ph     H     OH, OH                                          3967 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               OH, OH                                          3968 NH(CNH)NH.sub.2                                                                             Ph     H     (+)-pin                                         3969 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               (+)-pin                                         3970 NH(CNH)NH.sub.2                                                                             Ph     H     OH, OH                                          3971 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               OH, OH                                          3972 OMe          Ph     CH.sub.3                                                                             (+)-pin                                         3973 NH(CNH)H     Ph     CH.sub.3                                                                             (+)-pin                                         3974 OMe          Ph     CH.sub.3                                                                             OH, OH                                          3975 NH(CNH)H     Ph     CH.sub.3                                                                             OH, OH                                          ______________________________________                                    

                  TABLE 24                                                         ______________________________________                                          ##STR119##                                                                    Ex   X            R.sup.13                                                                              R.sup.14                                                                             Y.sup.1 Y.sup.2                                                                       Phys. Data                               ______________________________________                                         3980 CH.sub.2 NH.sub.2                                                                           Ph     H     (+)-pin                                         3981 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               (+)-pin                                         3982 CH.sub.2 NH.sub.2                                                                           Ph     H     OH, OH                                          3983 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               OH, OH                                          3984 NH(CNH)NH.sub.2                                                                             Ph     H     (+)-pin                                         3985 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               (+)-pin                                         3986 NH(CNH)NH.sub.2                                                                             Ph     H     OH, OH                                          3987 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               OH, OH                                          3988 OMe          Ph     CH.sub.3                                                                             (+)-pin                                         3989 NH(CNH)H     Ph     CH.sub.3                                                                             (+)-pin                                         3990 OMe          Ph     CH.sub.3                                                                             OH, OH                                          3991 NH(CNH)H     Ph     CH.sub.3                                                                             OH, OH                                          ______________________________________                                    

                  TABLE 25                                                         ______________________________________                                          ##STR120##                                                                                                               Phys.                               Ex   X            R.sup.13                                                                              R.sup.14                                                                             R.sup.15                                                                            Y.sup.1 Y.sup.2                                                                       Data                                ______________________________________                                         3996 CH.sub.2 NH.sub.2                                                                           Ph     H     H    (+)-pin                                    3997 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               H    (+)-pin                                    3998 CH.sub.2 NH.sub.2                                                                           Ph     H     H    OH, OH                                     3999 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               H    OH, OH                                     4000 NH(CNH)NH.sub.2                                                                             Ph     H     H    (+)-pin                                    4001 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               H    (+)-pin                                    4002 NH(CNH)NH.sub.2                                                                             Ph     H     H    OH, OH                                     4003 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               H    OH, OH                                     4004 OMe          Ph     CH.sub.3                                                                             H    (+)-pin                                    4005 NH(CNH)H     Ph     CH.sub.3                                                                             H    (+)-pin                                    4006 OMe          Ph     CH.sub.3                                                                             H    OH, OH                                     4007 NH(CNH)H     Ph     CH.sub.3                                                                             H    OH, OH                                     ______________________________________                                    

                  TABLE 26                                                         ______________________________________                                          ##STR121##                                                                                                               Phys.                               Ex   X            R.sup.13                                                                              R.sup.14                                                                             R.sup.15                                                                            Y.sup.1 Y.sup.2                                                                       Data                                ______________________________________                                         4012 CH.sub.2 NH.sub.2                                                                           Ph     H     H    (+)-pin                                    4013 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               H    (+)-pin                                    4014 CH.sub.2 NH.sub.2                                                                           Ph     H     H    OH, OH                                     4015 CH.sub.2 NH.sub.2                                                                           Ph     methyl                                                                               H    OH, OH                                     4016 CH.sub.2 NH.sub.2                                                                           Ph     H     Ph   (+)-pin                                    4017 CH.sub.2 NH.sub.2                                                                           Ph     H     Ph   OH, OH                                     4018 NH(CNH)NH.sub.2                                                                             Ph     H     H    (+)-pin                                    4019 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               H    (+)-pin                                    4020 NH(CNH)NH.sub.2                                                                             Ph     H     H    OH, OH                                     4021 NH(CNH)NH.sub.2                                                                             Ph     methyl                                                                               H    OH, OH                                     4022 NH(CNH)NH.sub.2                                                                             Ph     H     Ph   (+)-pin                                    4023 NH(CNH)NH.sub.2                                                                             Ph     H     Ph   OH, OH                                     4024 OMe          Ph     CH.sub.3                                                                             H    (+)-pin                                    4025 NH(CNH)H     Ph     CH.sub.3                                                                             H    (+)-pin                                    4026 OMe          Ph     CH.sub.3                                                                             H    OH, OH                                     4027 NH(CNH)H     Ph     CH.sub.3                                                                             H    OH, OH                                     ______________________________________                                    

                                      TABLE 27                                     __________________________________________________________________________      ##STR122##                                                                                                  Phys.                                            Ex X        R.sup.13                                                                          R.sup.14                                                                           R.sup.15                                                                          R.sup.16                                                                          Y.sup.1 Y.sup.2                                                                     Data                                             __________________________________________________________________________     4032                                                                              CH.sub.2 NH.sub.2                                                                       Ph H   H  H  (+)-pin                                               4033                                                                              CH.sub.2 NH.sub.2                                                                       Ph methyl                                                                             H  H  (+)-pin                                               4034                                                                              CH.sub.2 NH.sub.2                                                                       Ph H   H  H  OH, OH                                                4035                                                                              CH.sub.2 NH.sub.2                                                                       Ph methyl                                                                             H  H  OH, OH                                                4036                                                                              NH(CNH)NH.sub.2                                                                         Ph H   H  H  (+)-pin                                               4037                                                                              NH(CNH)NH.sub.2                                                                         Ph methyl                                                                             H  H  (+)-pin                                               4038                                                                              NH(CNH)NH.sub.2                                                                         Ph H   H  H  OH, OH                                                4039                                                                              NH(CNH)NH.sub.2                                                                         Ph methyl                                                                             H  H  OH, OH                                                4040                                                                              NH(CNH)NH.sub.2                                                                         Ph H   CH.sub.3                                                                          CH.sub.3                                                                          (+)-pin                                               4041                                                                              NH(CNH)NH.sub.2                                                                         Ph H   CH.sub.3                                                                          CH.sub.3                                                                          OH, OH                                                4042                                                                              OMe      Ph CH.sub.3                                                                           H  H  (+)-pin                                               4043                                                                              NH(CNH)H Ph CH.sub.3                                                                           H  H  (+)-pin                                               4044                                                                              OMe      Ph CH.sub.3                                                                           H  H  OH, OH                                                4045                                                                              NH(CNH)H Ph CH.sub.3                                                                           H  H  OH, OH                                                __________________________________________________________________________

                                      TABLE 28                                     __________________________________________________________________________      ##STR123##                                                                    Ex X        R.sup.13                                                                          R.sup.14                                                                             R.sup.15                                                                          R.sup.16                                                                          Y.sup.1 Y.sup.2                                                                     Phys. Data                                     __________________________________________________________________________     4050                                                                              CH.sub.2 NH.sub.2                                                                       Ph CH.sub.2 CO.sub.2 H                                                                  H  H  (+)-pin                                             4051                                                                              CH.sub.2 NH.sub.2                                                                       Ph methyl                                                                               H  H  (+)-pin                                             4052                                                                              CH.sub.2 NH.sub.2                                                                       Ph CH.sub.2 CO.sub.2 H                                                                  H  H  OH, OH                                              4053                                                                              CH.sub.2 NH.sub.2                                                                       Ph methyl                                                                               H  H  OH, OH                                              4054                                                                              NH(CNH)NH.sub.2                                                                         Ph CH.sub.2 CN                                                                          H  H  (+)-pin                                             4055                                                                              NH(CNH)NH.sub.2                                                                         Ph methyl                                                                               H  H  (+)-pin                                             4056                                                                              NH(CNH)NH.sub.2                                                                         Ph CH.sub.2 CN                                                                          H  H  OH, OH                                              4057                                                                              NH(CNH)NH.sub.2                                                                         Ph methyl                                                                               H  H  OH, OH                                              4058                                                                              NH(CNH)NH.sub.2                                                                         Ph CH.sub.3                                                                             CH.sub.3                                                                          H  (+)-pin                                             4059                                                                              NH(CNH)NH.sub.2                                                                         Ph CH.sub.3                                                                             CH.sub.3                                                                          H  OH, OH                                              4060                                                                              OMe      Ph CH.sub.3                                                                             H  H  (+)-pin                                             4061                                                                              NH(CNH)H Ph CH.sub.3                                                                             H  H  (+)-pin                                             4062                                                                              OMe      Ph CH.sub.3                                                                             H  H  OH, OH                                              4063                                                                              NH(CNH)H Ph CH.sub.3                                                                             H  H  OH, OH                                              4064                                                                              CH.sub.2 NH.sub.2                                                                       Ph H     H  H  (+)-pin                                             4065                                                                              CH.sub.2 NH.sub.2                                                                       Ph H     H  H  OH, OH                                              __________________________________________________________________________

                                      TABLE 29                                     __________________________________________________________________________      ##STR124##                                                                    Ex X        R.sup.13                                                                          R.sup.14                                                                           R.sup.15                                                                          R.sup.16                                                                          Y.sup.1 Y.sup.2                                                                     Phys. Data                                       __________________________________________________________________________     4070                                                                              CH.sub.2 NH.sub.2                                                                       Ph H   H  H  (+)-pin                                               4071                                                                              CH.sub.2 NH.sub.2                                                                       Ph methyl                                                                             H  H  (+)-pin                                               4072                                                                              CH.sub.2 NH.sub.2                                                                       Ph H   H  H  OH, OH                                                4073                                                                              CH.sub.2 NH.sub.2                                                                       Ph methyl                                                                             H  H  OH, OH                                                4074                                                                              NH(CNH)NH.sub.2                                                                         Ph H   H  H  (+)-pin                                               4075                                                                              NH(CNH)NH.sub.2                                                                         Ph methyl                                                                             H  H  (+)-pin                                               4076                                                                              NH(CNH)NH.sub.2                                                                         Ph H   H  H  OH, OH                                                4077                                                                              NH(CNH)NH.sub.2                                                                         Ph methyl                                                                             H  H  OH, OH                                                4078                                                                              NH(CNH)NH.sub.2                                                                         Ph CH.sub.3                                                                           CH.sub.3                                                                          H  (+)-pin                                               4079                                                                              NH(CNH)NH.sub.2                                                                         Ph CH.sub.3                                                                           CH.sub.3                                                                          H  OH, OH                                                4080                                                                              OMe      Ph H   H  OH (+)-pin                                               4081                                                                              NH(CNH)H Ph H   H  F  (+)-pin                                               4082                                                                              OMe      Ph H   H  Me OH, OH                                                4083                                                                              NH(CNH)H Ph H   H  Et OH, OH                                                __________________________________________________________________________

                                      TABLE 30                                     __________________________________________________________________________      ##STR125##                                                                                                      Phys.                                        Ex X        R.sup.13                                                                           R.sup.14                                                                          R.sup.15                                                                              R.sup.16                                                                          Y.sup.1 Y.sup.2                                                                     Data                                         __________________________________________________________________________     4088                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  H      Cl (+)-pin                                           4089                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  methyl H  (+)-pin                                           4090                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                           H  (+)-pin                                           4091                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                         H  (+)-pin                                           4092                                                                              CH.sub.2 NH.sub.2                                                                       PbCH.sub.2                                                                         H  CH.sub.2 NC                                                                           H  (+)-pin                                           4093                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                     H  (+)-pin                                           4094                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                   H  (+)-pin                                           4095                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                   H  (+)-pin                                           4096                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  H      NO.sub.2                                                                          OH, OH                                            4097                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  methyl H  OH, OH                                            4098                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                           H  OH, OH                                            4099                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                         H  OH, CH                                            4100                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                           H  OH, OH                                            4101                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                     H  OH, OH                                            4102                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                   H  OH, OH                                            4103                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                   H  OH, OH                                            4104                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  H      H  (+)-pin                                           4105                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  methyl H  (+)-pin                                           4106                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                           H  (+)-pin                                           4107                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                         H  (+)-pin                                           4108                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                           H  (+)-pin                                           4109                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                     H  (+)-pin                                           4110                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                   H  (+)-pin                                           4111                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                   H  (+)-pin                                           4112                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  H      H  OH, OH                                            4113                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  methyl H  OH, OH                                            4114                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                           H  OH, OH                                            4115                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                         H  OH, OH                                            4116                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                           H  OH, OH                                            4117                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                     H  OH, OH                                            4118                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                   H  OH, OH                                            4119                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                   H  OH, OH                                            __________________________________________________________________________

                                      TABLE 31                                     __________________________________________________________________________      ##STR126##                                                                    Ex X        R.sup.13                                                                           R.sup.14                                                                          R.sup.15                                                                              Y.sup.1 Y.sup.2                                                                     Phys. Data                                      __________________________________________________________________________     4124                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  H      (+)-pin                                              4125                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  methyl (+)-pin                                              4126                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                           (+)-pin                                              4127                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                         (+)-pin                                              4128                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                           (+)-pin                                              4129                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                              4130                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                              4131                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                              4132                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  H      OH, OH                                               4133                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  methyl OH, OH                                               4134                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                           OH, OH                                               4135                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                         OH, OH                                               4136                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                           OH, OH                                               4137                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                     OH, OH                                               4138                                                                              CH.sub.2 NH.sub.2                                                                       PbCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                               4139                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                               4140                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  H      (+)-pin                                              4141                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  methyl (+)-pin                                              4142                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                           (+)-pin                                              4143                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                         (+)-pin                                              4144                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                           (+)-pin                                              4145                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                              4146                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                              4147                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                              4148                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  H      OH, OH                                               4149                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  methyl OH, OH                                               4150                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                           OH, OH                                               4151                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                         OH, OH                                               4152                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                           OH, OH                                               4153                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                     OH, OH                                               4154                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                               4155                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                               __________________________________________________________________________

                                      TABLE 32                                     __________________________________________________________________________      ##STR127##                                                                    Ex X        R.sup.13                                                                           R.sup.15                                                                          R.sup.14                                                                              Y.sup.1 Y.sup.2                                                                     Phys. Data                                      __________________________________________________________________________     4160                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  H      (+)-pin                                              4161                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         Cl H      (+)-pin                                              4162                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  methyl (+)-pin                                              4163                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                           (+)-pin                                              4164                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         Cl CH.sub.2 CN                                                                           (+)-pin                                              4165                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                         (+)-pin                                              4166                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                           (+)-pin                                              4167                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                              4168                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                              4169                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                              4170                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  H      OH, OH                                               4171                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         Cl H      OH, OH                                               4172                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  methyl OH, OH                                               4173                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                           OH, OH                                               4174                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         Cl CH.sub.2 CN                                                                           OH, OH                                               4175                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                         OH, OH                                               4176                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                           OH, OH                                               4177                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                     OH, OH                                               4178                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                               4179                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                               4180                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  H      (+)-pin                                              4181                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  methyl (+)-pin                                              4182                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                           (+)-pin                                              4183                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                         (+)-pin                                              4184                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                           (+)-pin                                              4185                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                              4186                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                              4187                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                              4188                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  H      OH, OH                                               4189                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  methyl OH, OH                                               4190                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 CN                                                                           OH, OH                                               4191                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 COOH                                                                         OH, OH                                               4192                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 NC                                                                           OH, OH                                               4193                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 NO.sub.2                                                                     OH, OH                                               4194                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                               4195                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                               __________________________________________________________________________

                                      TABLE 33                                     __________________________________________________________________________      ##STR128##                                                                                                     Phys.                                         Ex  X         R.sup.13                                                                            R.sup.14                                                                               Y.sup.1 Y.sup.2                                                                      Data                                          __________________________________________________________________________     4200                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                             4201                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                             4202                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                             4203                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                             4204                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                             4205                                                                               CH.sub.2 NH.sub.2                                                                        PbCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                             4206                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                             4207                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                             4208                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                             4209                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                              4210                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                              4211                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                              4212                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                              4213                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                              4214                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                              4215                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                              4216                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                              4217                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                              4218                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                             4219                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                             4220                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                             4221                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                             4222                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                             4223                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                       4224                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                             4225                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                             4226                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                             4227                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                             4228                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                              4229                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                              4230                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                              4231                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                              4232                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                              4233                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                              4234                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                              4235                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                              4236                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                              4237                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                              __________________________________________________________________________

                  TABLE 34                                                         ______________________________________                                          ##STR129##                                                                    Ex   X            R.sup.13   Y.sup.1 Y.sup.2                                                                       Phys. Data                                 ______________________________________                                              m = 1                                                                     4242 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                           4243 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                            4244 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                           4245 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                            4246 OMe          PhCH.sub.2 (+)-pin                                           4247 OMe          PhCH.sub.2 OH, OH                                            4248 NH(CNH)H     PhCH.sub.2 (+)-pin                                           4249 NH(CNH)H     PhCH.sub.2 OH, OH                                            4250 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                                                               DB                                         4251 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4252 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4253 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4254 OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4255 OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4256 NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4257 NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH DC                                         4258 CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                           4259 CH.sub.2 NH.sub.2                                                                           Ph         OH, CH                                            4260 NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                           4261 NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                            4262 OMe          Ph         (+)-pin                                           4263 OMe          Ph         OH, OH                                            4264 NH(CNH)H     Ph         (+)-pin                                           4265 NH(CNH)H     Ph         OH, OH                                            4266 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2 S                                                                     (+)-pin                                           4267 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 S                                                                              (+)-pin                                           4268 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2 S                                                                     OH, OH                                            4269 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 S                                                                              OH, OH                                            4270 m = 2                                                                     4271 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                           4272 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                            4273 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                           4274 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                            4275 OMe          PhCH.sub.2 (+)-pin                                           4276 OMe          PhCH.sub.2 OH, OH                                            4277 NH(CNH)H     PhCH.sub.2 (+)-pin                                           4278 NH(CNH)H     PhCH.sub.2 OH, OH                                            4279 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4280 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4281 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4282 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4283 OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4284 OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4285 NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4286 NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4287 CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                           4288 CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                            4289 NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                           4290 NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                            4291 OMe          Ph         (+)-pin                                           4292 ome          Ph         OH, OH                                            4293 NH(CNH)H     Ph         (+)-pin                                           4294 NH(CNH)H     Ph         OH, OH                                            ______________________________________                                          DB. HRMS Calc'd. 495.3255, Found 495.3257                                      DC. HRMS Calc'd. 467.2442, Found 467.2950                                

                  TABLE 35                                                         ______________________________________                                          ##STR130##                                                                    Ex   X            R.sup.13   Y.sup.1 Y.sup.2                                                                       Phys. Data                                 ______________________________________                                         m = 1                                                                          4299 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                           4300 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                            4301 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                           4302 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                            4303 OMe          PhCH.sub.2 (+)-pin                                           4304 OMe          PhCH.sub.2 OH, OH                                            4305 NH(CNH)H     PhCH.sub.2 (+)-pin                                           4306 NH(CNH)H     PhCH.sub.2 OH, OH                                            4307 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                                                               DE                                         4308 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4309 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4310 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4311 OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4312 OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4313 NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4314 NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4315 CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                           4316 CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                            4317 NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                           4318 NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                            4319 OMe          Ph         (+)-pin                                           4320 OMe          Ph         OH, OH                                            4321 NH(CNH)H     Ph         (+)-pin                                           4322 NH(CNH)H     Ph         OH, OH                                            4323 m = 2                                                                     4324 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                           4325 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                            4326 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                           4327 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                            4328 OMe          PhCH.sub.2 (+)-pin                                           4329 OMe          PhCH.sub.2 OH, OH                                            4330 NH(CNH)H     PhCH.sub.2 (+)-pin                                           4331 NH(CNH)H     PhCH.sub.2 OH, OH                                            4332 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4333 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4334 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4335 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4336 OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4337 OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4338 NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           4339 NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            4340 CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                           4341 CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                            4342 NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                           4343 NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                            4344 OMe          Ph         (+)-pin                                           4345 OMe          Ph         OH, OH                                            4346 NH(CNH)H     Ph         (+)-pin                                           4347 NH(CNH)H     Ph         OH, OH                                            ______________________________________                                          DE. HRMS Calc'd. 495.3255, Found 495.3249                                

                                      TABLE 36                                     __________________________________________________________________________      ##STR131##                                                                                                     Phys.                                         Ex  X         R.sup.13                                                                            R.sup.14                                                                               Y.sup.1 Y.sup.2                                                                      Data                                          __________________________________________________________________________     m = 1                                                                          4348                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                             4349                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                             4350                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                             4351                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                             4352                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                             4353                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                             4354                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                             4355                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                             4356                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                              4357                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                              4358                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                              4359                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                              4360                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                              4361                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                              4362                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                              4363                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                              4364                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                             4365                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                             4366                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                             4367                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                             4368                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                             4369                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                             4370                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                             4371                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                             4372                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                             4373                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                             4374                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       H, OH                                               4375                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                              4376                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                              4377                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                              4378                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                              4379                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                              4380                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                              4381                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                              4382                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                              4383                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                              4384                                                                               m = 2                                                                      4385                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                             4386                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                             4387                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                             4388                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                             4389                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                             4390                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                             4391                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                             4392                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                             4393                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                              4394                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                              4395                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                              4396                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                              4397                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                              4398                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                              4399                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                              4400                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                              4401                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2   (+)-pin                                             4402                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          ethyl   (+)-pin                                             4403                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                             4404                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                             4405                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                             4406                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                             4407                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                             4408                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                             4409                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                             4410                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                             4411                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2   OH, OH                                              4412                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          ethyl   OH, OH                                              4413                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                              4414                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                              4415                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                              4416                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                              4417                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                              4418                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                              4419                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                              4420                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                              4421                                                                               m = 0                                                                      4422                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                             4423                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                             4424                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                             4425                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                             4426                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                             4427                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                             4428                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                             4429                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                             4430                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                              4431                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                              4432                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                              4433                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                              4434                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                              4435                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                              4436                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                              4437                                                                               CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                              4438                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                             4439                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                             4440                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                             4441                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                             4442                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                             4443                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                             4444                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                             4445                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                             4446                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                             4447                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                             4448                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       H, OH                                               4449                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                              4450                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                              4451                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                              4452                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                              4453                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                              4454                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                              4455                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                              4456                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                              4457                                                                               NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                              __________________________________________________________________________

                                      TABLE 37                                     __________________________________________________________________________      ##STR132##                                                                    Ex X         R.sup.13                                                                            R.sup.14                                                                               Y.sup.1 Y.sup.2                                                                     Phys. Data                                      __________________________________________________________________________        m = 1                                                                       4462                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4463                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4464                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4465                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4466                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4467                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4468                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4469                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4470                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4471                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4472                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4473                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4474                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4475                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4476                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4477                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4478                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4479                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4480                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4481                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4482                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4483                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4484                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4485                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4486                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4487                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4488                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4489                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4490                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4491                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4492                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4493                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4494                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4495                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4496                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4497                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4498                                                                              m = 2                                                                       4499                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4500                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4501                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4502                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4503                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4504                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4505                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4506                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4507                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4508                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4509                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4510                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4511                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4512                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4513                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4514                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4515                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4516                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4517                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4518                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4519                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4520                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4521                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4522                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4523                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4524                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4525                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4526                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4527                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4528                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4529                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4530                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4531                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4532                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4533                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4534                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               m = 0                                                                          4535                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4536                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4537                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4538                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4539                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4540                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4541                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4542                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4543                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4544                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4545                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4546                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4547                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4548                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4549                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4550                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4551                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4552                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4553                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4554                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4555                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4556                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4557                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4558                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4559                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4560                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4561                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4562                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4563                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4564                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4565                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4566                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4567                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4568                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4569                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4570                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               __________________________________________________________________________

                                      TABLE 38                                     __________________________________________________________________________      ##STR133##                                                                    Ex X         R.sup.13                                                                            R.sup.14                                                                               Y.sup.1 Y.sup.2                                                                     Phys. Data                                      __________________________________________________________________________        m = 1                                                                       4575                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4576                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4577                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4578                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4579                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4580                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4581                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4582                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4583                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4584                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4585                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4586                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4587                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4588                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4589                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4590                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4591                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4592                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4593                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4594                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4595                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4596                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4597                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4598                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4599                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4600                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4601                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4602                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4603                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4604                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4605                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4606                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4607                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4608                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4609                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4610                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               m = 0                                                                          4611                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4612                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4613                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4614                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4615                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4616                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4617                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4618                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4619                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4620                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4621                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4622                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4623                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4624                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4625                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4626                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4627                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4628                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4629                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4630                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4631                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4632                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4633                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4634                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4635                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4636                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4637                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4638                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4639                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4640                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4641                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4642                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4643                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4644                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4645                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4646                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               __________________________________________________________________________

                                      TABLE 39                                     __________________________________________________________________________      ##STR134##                                                                    Ex X         R.sup.13                                                                            R.sup.14                                                                               Y.sup.1 Y.sup.2                                                                     Phys. Data                                      __________________________________________________________________________        m = 1                                                                       4651                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4652                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4653                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4654                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4655                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4656                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4657                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4658                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4659                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4660                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4661                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4662                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4663                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4664                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4665                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4666                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4667                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4668                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4669                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4670                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4671                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4672                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4673                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4674                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4675                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4676                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4677                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4678                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4679                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4680                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4681                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4682                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4683                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4684                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4685                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4686                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               m = 0                                                                          4687                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4688                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4689                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4690                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4691                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4692                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4693                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4694                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4695                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4696                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4697                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4698                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4699                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4700                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4701                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4702                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4703                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4704                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4705                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4706                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4707                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4708                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4709                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4710                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4711                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4712                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4713                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4714                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4715                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4716                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4717                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4718                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4719                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4720                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4721                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4722                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               __________________________________________________________________________

                                      TABLE 40                                     __________________________________________________________________________      ##STR135##                                                                    Ex X         R.sup.13                                                                            R.sup.14                                                                               Y.sup.1 Y.sup.2                                                                     Phys. Data                                      __________________________________________________________________________        m = 1                                                                       4727                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4728                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4729                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4730                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4731                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4732                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4733                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4734                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4735                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4736                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4737                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4738                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4739                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4740                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4741                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4742                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4743                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4744                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4745                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4746                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4747                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4748                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4749                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4750                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4751                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4752                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4753                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4754                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4755                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4756                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4757                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4758                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4759                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4760                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4761                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4762                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               m = 0                                                                          4763                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4764                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4765                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4766                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4767                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4768                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4769                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4770                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4771                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4772                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4773                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4774                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4775                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4776                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4777                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4778                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4779                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4780                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4781                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4782                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4783                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4784                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4785                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4786                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4787                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4788                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4789                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4790                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4791                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4792                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4793                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4794                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4795                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4796                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4797                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4798                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               __________________________________________________________________________

                                      TABLE 41                                     __________________________________________________________________________      ##STR136##                                                                    Ex X         R.sup.13                                                                            R.sup.14                                                                               Y.sup.1 Y.sup.2                                                                     Phys. Data                                      __________________________________________________________________________        m = 1                                                                       4803                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4804                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4805                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4806                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4807                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4808                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4809                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4810                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4811                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4812                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4813                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4814                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4815                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4816                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4817                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, CH                                               4818                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4819                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4820                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4821                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4822                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4823                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4824                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4825                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4826                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4827                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4828                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4829                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4830                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4831                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4832                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4833                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4834                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4835                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4836                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4837                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4838                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               m = 0                                                                          4839                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4840                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4841                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4842                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4843                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4844                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4845                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4846                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4847                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4848                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4849                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4850                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4851                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4852                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4853                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4854                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4855                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4856                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4857                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4858                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4859                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4860                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4861                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4862                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4863                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4864                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4865                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4866                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4867                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4868                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4869                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4870                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4871                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4872                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4873                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4874                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               __________________________________________________________________________

                                      TABLE 42                                     __________________________________________________________________________      ##STR137##                                                                    Ex X         R.sup.13                                                                            R.sup.14                                                                               Y.sup.1 Y.sup.2                                                                     Phys. Data                                      __________________________________________________________________________        m = 1                                                                       4879                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4880                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4881                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4882                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4883                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4884                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4885                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4886                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4887                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4888                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4889                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4890                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4891                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4892                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4893                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4894                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4895                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4896                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4897                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4898                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4899                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4900                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4901                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4902                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4903                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4904                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4905                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4906                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4907                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4908                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4909                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4910                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4911                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4912                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4913                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4914                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               m = 2                                                                          4915                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4916                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4917                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4918                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4919                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4920                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4921                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4922                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4923                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4924                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4925                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4926                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4927                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4928                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4929                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4930                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4931                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4932                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4933                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4934                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4935                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4936                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4937                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4938                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4939                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4940                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4941                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4942                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4943                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4944                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4945                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4946                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4947                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4948                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4949                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4950                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               m = 0                                                                          4951                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4952                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4953                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4954                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4955                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4956                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4957                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4958                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4959                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               4960                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               4961                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4962                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4963                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4964                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4965                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4966                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               4967                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              4968                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              4969                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4970                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              4971                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4972                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              4973                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4974                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4975                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4976                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4977                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               4978                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               4979                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               4980                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               4981                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               4982                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               4983                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               4984                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               4985                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               4986                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               __________________________________________________________________________

                                      TABLE 43                                     __________________________________________________________________________      ##STR138##                                                                    Ex X         R.sup.13                                                                            R.sup.14                                                                               Y.sup.1 Y.sup.2                                                                     Phys. Data                                      __________________________________________________________________________        m = 1                                                                       4991                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              4992                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              4993                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              4994                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              4995                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              4996                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              4997                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              4998                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              4999                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               5000                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               5001                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               5002                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               5003                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               5004                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               5005                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               5006                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               5007                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              5008                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              5009                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              5010                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              5011                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              5012                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              5013                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              5014                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              5015                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              5016                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              5017                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               5018                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               5019                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               5020                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               5021                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               5022                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               5023                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               5024                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               5025                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               5026                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               m = 2                                                                          5027                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              5028                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              5029                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              5030                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              5031                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              5032                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              5033                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              5034                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              5035                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               5036                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               5037                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               5038                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               5039                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               5040                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               5041                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               5042                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               5043                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              5044                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              5045                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              5046                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              5047                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              5048                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              5049                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              5050                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              5051                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              5052                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              5053                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               5054                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               5055                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               5056                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               5057                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               5058                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               5059                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               5060                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               5061                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               5062                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               m = 0                                                                          5063                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              5064                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              5065                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              5066                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              5067                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              5068                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              5069                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              5070                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              5071                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               5072                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               5073                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               5074                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               5075                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               5076                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               5077                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               5078                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               5079                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              5080                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              5081                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              5082                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              5083                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              5084                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              5085                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              5086                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              5087                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              5088                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              5089                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               5090                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               5091                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               5092                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               5093                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               5094                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               5095                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               5096                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               5097                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               5098                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               __________________________________________________________________________

                                      TABLE 44                                     __________________________________________________________________________      ##STR139##                                                                    Ex X         R.sup.13                                                                            R.sup.14                                                                               Y.sup.1 Y.sup.2                                                                     Phys. Data                                      __________________________________________________________________________        m = 1                                                                       5103                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              5104                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              5105                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              5106                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              5107                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              5108                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              5109                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              5110                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              5111                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               5112                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               5113                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               5114                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               5115                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               5116                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               5117                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               5118                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               5119                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              5120                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              5121                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              5122                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              5123                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              5124                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              5125                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              5126                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              5127                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              5128                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              5129                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               5130                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               5131                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               5132                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               5133                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               5134                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               5135                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               5136                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               5137                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               5138                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               m = 2                                                                          5139                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              5140                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              5141                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              5142                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              5143                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              5144                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              5145                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              5146                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              5147                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               5148                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               5149                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               5150                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               5151                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               5152                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               5153                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               5154                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               5155                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              5156                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              5157                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              5158                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              5159                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              5160                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              5161                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              5162                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              5163                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              5164                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              5165                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               5166                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               5167                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               5168                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               5169                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               5170                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               5171                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               5172                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               5173                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               5174                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               m = 0                                                                          5175                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       (+)-pin                                              5176                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  (+)-pin                                              5177                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              5178                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              5179                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              5180                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              5181                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              5182                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              5183                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          H       OH, OH                                               5184                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          methyl  OH, OH                                               5185                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               5186                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               5187                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               5188                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               5189                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               5190                                                                              CH.sub.2 NH.sub.2                                                                        PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               5191                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       (+)-pin                                              5192                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  (+)-pin                                              5193                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            (+)-pin                                              5194                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    (+)-pin                                              5195                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          (+)-pin                                              5196                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                              5197                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            (+)-pin                                              5198                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      (+)-pin                                              5199                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    (+)-pin                                              5200                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    (+)-pin                                              5201                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          H       OH, OH                                               5202                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          methyl  OH, OH                                               5203                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 CN                                                                            OH, OH                                               5204                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 CN                                                                    OH, OH                                               5205                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 COOH                                                                          OH, OH                                               5206                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 COOH                                                                  OH, OH                                               5207                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NC                                                                            OH, OH                                               5208                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 NO.sub.2                                                                      OH, OH                                               5209                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          (CH.sub.2).sub.2 OH                                                                    OH, OH                                               5210                                                                              NH(CNH)NH.sub.2                                                                          PhCH.sub.2                                                                          CH.sub.2 SOCH.sub.3                                                                    OH, OH                                               __________________________________________________________________________

                  TABLE 45                                                         ______________________________________                                          ##STR140##                                                                    Ex   X            R.sup.13   Y.sup.1 Y.sup.2                                                                       Phys. Data                                 ______________________________________                                              m = 1                                                                     5215 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                           5216 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                            5217 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                           5218 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                            5219 OMe          PhCH.sub.2 (+)-pin                                           5220 OMe          PhCH.sub.2 OH, OH                                            5221 NH(CNH)H     PhCH.sub.2 (+)-pin                                           5222 NH(CNH)H     PhCH.sub.2 OH, OH                                            5223 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           5224 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            5225 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           5226 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            5227 OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           5228 OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            5229 NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           5230 NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            5231 CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                           5232 CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                            5233 NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                           5234 NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                            5235 OMe          Ph         (+)-pin                                           5236 OMe          Ph         OH, OH                                            5237 NH(CNH)H     Ph         (+)-pin                                           5238 NH(CNH)H     Ph         OH, OH                                            m = 0                                                                          5239 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 (+)-pin                                           5240 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 OH, OH                                            5241 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 (+)-pin                                           5242 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 OH, OH                                            5243 OMe          PhCH.sub.2 (+)-pin                                           5244 OMe          PhCH.sub.2 OH, OH                                            5245 NH(CNH)H     PhCH.sub.2 (+)-pin                                           5246 NH(CNH)H     PhCH.sub.2 OH, OH                                            5247 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           5248 CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            5249 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           5250 NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            5251 OMe          PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           5252 OMe          PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            5253 NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       (+)-pin                                           5254 NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                       OH, OH                                            5255 CH.sub.2 NH.sub.2                                                                           Ph         (+)-pin                                           5256 CH.sub.2 NH.sub.2                                                                           Ph         OH, OH                                            5257 NH(CNH)NH.sub.2                                                                             Ph         (+)-pin                                           5258 NH(CNH)NH.sub.2                                                                             Ph         OH, OH                                            5259 OMe          Ph         (+)-pin                                           5260 OMe          Ph         OH, OH                                            5261 NH(CNH)H     Ph         (+)-pin                                           5262 NH(CNH) H    Ph         OH, OH                                            ______________________________________                                    

                  TABLE 46                                                         ______________________________________                                          ##STR141##                                                                    Ex    X            R.sup.13  Y.sup.1 Y.sup.2                                                                        Phys. Data                                ______________________________________                                         m = 1                                                                          5267  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2                                                                               (+)-pin                                           5268  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2                                                                               OH, OH                                            5269  NH(CNH)NH.sub.2                                                                             PhCH.sub.2                                                                               (+)-pin                                           5270  NH(CNH)NH.sub.2                                                                             PhCH.sub.2                                                                               OH, OH                                            5271  OMe          PhCH.sub.2                                                                               (+)-pin                                           5272  OMe          PhCH.sub.2                                                                               OH, OH                                            5273  NH(CNH)H     PhCH.sub.2                                                                               (+)-pin                                           5274  NH(CNH)H     PhCH.sub.2                                                                               OH, OH                                            5275  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5276  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5277  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5278  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5279  OMe          PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5280  OMe          PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5281  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5282  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5283  CH.sub.2 NH.sub.2                                                                           Ph        (+)-pin                                           5284  CH.sub.2 NH.sub.2                                                                           Ph        OH, OH                                            5285  NH(CNH)NH.sub.2                                                                             Ph        (+)-pin                                           5286  NH(CNH)NH.sub.2                                                                             Ph        OH, OH                                            5287  OMe          Ph        (+)-pin                                           5288  OMe          Ph        OH, OH                                            5289  NH(CNH)H     Ph        (+)-pin                                           5290  NH(CNH)H     Ph        OH, OH                                            m = 0                                                                          5291  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2                                                                               (+)-pin                                           5292  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2                                                                               OH, OH                                            5293  NH(CNH)NH.sub.2                                                                             PhCH.sub.2                                                                               (+)-pin                                           5294  NH(CNH)NH.sub.2                                                                             PhCH.sub.2                                                                               OH, OH                                            5295  OMe          PhCH.sub.2                                                                               (+)-pin                                           5296  OMe          PhCH.sub.2                                                                               OH, OH                                            5297  NH(CNH)H     PhCH.sub.2                                                                               (+)-pin                                           5298  NH(CNH)H     PhCH.sub.2                                                                               OH, OH                                            5299  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5300  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5301  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5302  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5303  OMe          PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5304  OMe          PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5305  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5306  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5307  CH.sub.2 NH.sub.2                                                                           Ph        (+)-pin                                           5308  CH.sub.2 NH.sub.2                                                                           Ph        OH, OH                                            5309  NH(CNH)NH.sub.2                                                                             Ph        (+)-pin                                           5310  NH(CNH)NH.sub.2                                                                             Ph        OH, OH                                            5311  OMe          Ph        (+)-pin                                           5312  OMe          Ph        OH, OH                                            5313  NH(CNH)H     Ph        (+)-pin                                           5314  NH(CNH)H     Ph        OH, OH                                            ______________________________________                                    

                  TABLE 47                                                         ______________________________________                                          ##STR142##                                                                    Ex    X            R.sup.13  Y.sup.1 Y.sup.2                                                                        Phys. Data                                ______________________________________                                         m = 1                                                                          5319  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2                                                                               (+)-pin                                           5320  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2                                                                               OH, OH                                            5321  NH(CNH)NH.sub.2                                                                             PhCH.sub.2                                                                               (+)-pin                                           5322  NH(CNH)NH.sub.2                                                                             PhCH.sub.2                                                                               OH, OH                                            5323  OMe          PhCH.sub.2                                                                               (+)-pin                                           5324  OMe          PhCH.sub.2                                                                               OH, OH                                            5325  NH(CNH)H     PhCH.sub.2                                                                               (+)-pin                                           5326  NH(CNH)H     PhCH.sub.2                                                                               OH, OH                                            5327  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5328  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5329  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5330  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5331  OMe          PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5332  OMe          PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5333  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5334  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5335  CH.sub.2 NH.sub.2                                                                           Ph        (+)-pin                                           5336  CH.sub.2 NH.sub.2                                                                           Ph        OH, OH                                            5337  NH(CNH)NH.sub.2                                                                             Ph        (+)-pin                                           5338  NH(CNH)NH.sub.2                                                                             Ph        OH, OH                                            5339  OMe          Ph        (+)-pin                                           5340  OMe          Ph        OH, OH                                            5341  NH(CNH)H     Ph        (+)-pin                                           5342  NH(CNH)H     Ph        OH, OH                                            m = 0                                                                          5343  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2                                                                               (+)-pin                                           5344  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2                                                                               OH, OH                                            5345  NH(CNH)NH.sub.2                                                                             PhCH.sub.2                                                                               (+)-pin                                           5346  NH(CNH)NH.sub.2                                                                             PhCH.sub.2                                                                               OH, OH                                            5347  OMe          PhCH.sub.2                                                                               (+)-pin                                           5348  OMe          PhCH.sub.2                                                                               OH, OH                                            5349  NH(CNH)H     PhCH.sub.2                                                                               (+)-pin                                           5350  NH(CNH)H     PhCH.sub.2                                                                               OH, OH                                            5351  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5352  CH.sub.2 NH.sub.2                                                                           PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5353  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5354  NH(CNH)NH.sub.2                                                                             PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5355  OMe          PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5356  OMe          PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5357  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                      (+)-pin                                           5358  NH(CNH)H     PhCH.sub.2 CH.sub.2                                                                      OH, OH                                            5359  CH.sub.2 NH.sub.2                                                                           Ph        (+)-pin                                           5360  CH.sub.2 NH.sub.2                                                                           Ph        OH, OH                                            5361  NH(CNH)NH.sub.2                                                                             Ph        (+)-pin                                           5362  NH(CNH)NH.sub.2                                                                             Ph        OH, OH                                            5363  OMe          Ph        (+)-pin                                           5364  OMe          Ph        OH, OH                                            5365  NH(CNH)H     Ph        (+)-pin                                           5366  NH(CNH)H     Ph        OH, OH                                            ______________________________________                                    

                                      TABLE 48                                     __________________________________________________________________________      ##STR143##                                                                    Ex X        R.sup.13                                                                           R.sup.14                                                                             R.sup.15     Y.sup.1 Y.sup.2                                                                     Phys. Data                             __________________________________________________________________________     m = 1                                                                          5371                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     H            (+)-pin                                     5372                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     methyl       (+)-pin                                     5373                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     CH.sub.2 CN  (+)-pin                                     5374                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     CH.sub.2 COOH                                                                               (+)-pin                                     5375                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     CH.sub.2 NC  (+)-pin                                     5376                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     CH.sub.2 NO.sub.2                                                                           (+)-pin                                     5377                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     (CH.sub.2).sub.2 OH                                                                         (+)-pin                                     5378                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     CH.sub.2 SOCH.sub.3                                                                         (+)-pin                                     5379                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     H            OH, OH                                      5380                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     methyl       OH, OH                                      5381                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     CH.sub.2 CN  OH, OH                                      5382                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     CH.sub.2 COOH                                                                               OH, OH                                      5383                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     CH.sub.2 NC  OH, OH                                      5384                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     CH.sub.2 NO.sub.2                                                                           OH, OH                                      5385                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     (CH.sub.2).sub.2 OH                                                                         OH, OH                                      5386                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H     CH.sub.2 SOCH.sub.3                                                                         OH, OH                                      5387                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     H            (+)-pin                                     5388                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     methyl       (+)-pin                                     5389                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     CH.sub.2 CN  (+)-pin                                     5390                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     CH.sub.2 COOH                                                                               (+)-pin                                     5391                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     CH.sub.2 NC  (+)-pin                                     5392                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     CH.sub.2 NO.sub.2                                                                           (+)-pin                                     5393                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     (CH.sub.2).sub.2 OH                                                                         (+)-pin                                     5394                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     CH.sub.2 SOCH.sub.3                                                                         (+)-pin                                     5395                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     H            OH, OH                                      5396                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     methyl       OH, OH                                      5397                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     CH.sub.2 CN  OH, OH                                      5398                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     CH.sub.2 COOH                                                                               OH, OH                                      5399                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     CH.sub.2 NC  OH, OH                                      5400                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     CH.sub.2 NO.sub.2                                                                           OH, OH                                      5401                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     (CH.sub.2).sub.2 OH                                                                         OH, OH                                      5402                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H     CH.sub.2 SOCH.sub.3                                                                         OH, OH                                      5403                                                                              m = 0                                                                       5404                                                                              NH(CNH)NH.sub.2                                                                         H   H     3-(t-butyl-O.sub.2 CNH)Ph                                                                   (+)-pin                                                                             BS                                     5405                                                                              NH(CNH)NH.sub.2                                                                         H   H     3-(t-butyl-O.sub.2 CNH)Ph                                                                   OH, OH                                      5406                                                                              NH(CNH)NH.sub.2                                                                         H   H     3-(NH.sub.2)Ph                                                                              (+)-pin                                     5407                                                                              NH(CNH)NH.sub.2                                                                         H   H     3-(NH.sub.2)Ph                                                                              OH, OH                                      5408                                                                              NH(CNH)NH.sub.2                                                                         H   H     3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                                     5409                                                                              NH(CNH)NH.sub.2                                                                         H   H     3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                                      5410                                                                              NH(CNH)NH.sub.2                                                                         H   methyl                                                                               Ph           (+)-pin                                     5411                                                                              NH(CNH)NH.sub.2                                                                         H   methyl                                                                               Ph           OH, OH                                      5412                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 CN                                                                          Ph           (+)-pin                                     5413                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 CN                                                                          Ph           OH, OH                                      5414                                                                              NH(CNH)NH.sub.2                                                                         H   methyl                                                                               3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                                     5415                                                                              NH(CNH)NH.sub.2                                                                         H   methyl                                                                               3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                                      5416                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.3                                                                             2-(CH.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                                     5417                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.3                                                                             2-(CH.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                                      5418                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 CN                                                                          3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                                     5419                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 CN                                                                          3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                                      5420                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 CN                                                                          2-(CH.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                                     5421                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 CN                                                                          2-(CH.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                                      5422                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 COOH                                                                        3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                                     5423                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 COOH                                                                        3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                                      5424                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 COOH                                                                        2-(CH.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                                     5425                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 COOH                                                                        2-(CH.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                                      5426                                                                              NH(CNH)NH.sub.2                                                                         H   H     3-(t-butylOCONH)Ph                                                                          (+)-pin                                                                             BP                                     __________________________________________________________________________      BP. MS (M+H)+: Calc 610, Found 610.                                            BS. MS (M+H)+: Calc 610, Found 610                                       

                                      TABLE 49                                     __________________________________________________________________________      ##STR144##                                                                    Ex  X        R.sup.13                                                                            R.sup.14                                                                          R.sup.15                                                                              Y.sup.1 Y.sup.2                                                                     Phys. Data                                    __________________________________________________________________________     m = 1                                                                          5431                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  H      (+)-pin                                            5432                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  methyl (+)-pin                                            5433                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           (+)-pin                                            5434                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         (+)-pin                                            5435                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           (+)-pin                                            5436                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                            5437                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                            5438                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                            5439                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  H      OH, OH                                             5440                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  methyl OH, OH                                             5441                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           OH, OH                                             5442                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         OH, OH                                             5443                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           OH, OH                                             5444                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     OH, OH                                             5445                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                             5446                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                             5447                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  H      (+)-pin                                            5448                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  methyl (+)-pin                                            5449                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           (+)-pin                                            5450                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         (+)-pin                                            5451                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           (+)-pin                                            5452                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                            5453                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                            5454                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                            5455                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  H      OH, OH                                             5456                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  methyl OH, OH                                             5457                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           OH, OH                                             5458                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         OH, OH                                             5459                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           OH, OH                                             5460                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     OH, OH                                             5461                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                             5462                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                             m = 0                                                                          5463                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  H      (+)-pin                                            5464                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  methyl (+)-pin                                            5465                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           (+)-pin                                            5466                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         (+)-pin                                            5465                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           (+)-pin                                            5466                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                            5467                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                            5468                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                            5469                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  H      OH, OH                                             5470                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  methyl OH, OH                                             5471                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           OH, OH                                             5472                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         OH, OH                                             5473                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           OH, OH                                             5474                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     OH, OH                                             5475                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                             5476                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                             5477                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  H      (+)-pin                                            5478                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  methyl (+)-pin                                            5479                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           (+)-pin                                            5480                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         (+)-pin                                            5481                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           (+)-pin                                            5482                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                            5483                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                            5484                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                            5485                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  H      OH, OH                                             5486                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  methyl OH, OH                                             5487                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           OH, OH                                             5488                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         OH, OH                                             5489                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           OH, OH                                             5490                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     OH, OH                                             5491                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                             5492                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                             __________________________________________________________________________

                                      TABLE 50                                     __________________________________________________________________________      ##STR145##                                                                    Ex X        R.sup.13                                                                           R.sup.14                                                                              R.sup.15     Y.sup.1 Y.sup.2                                                                     Phys. Data                            __________________________________________________________________________     m = 1                                                                          5497                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      H            (+)-pin                                    5498                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      methyl       (+)-pin                                    5499                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      CH.sub.2 CN  (+)-pin                                    5500                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      CH.sub.2 COOH                                                                               (+)-pin                                    5501                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      CH.sub.2 NC  (+)-pin                                    5502                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      CH.sub.2 NO.sub.2                                                                           (+)-pin                                    5503                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      (CH.sub.2).sub.2 OH                                                                         (+)-pin                                    5504                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      CH.sub.2 SOCH.sub.3                                                                         (+)-pin                                    5505                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      H            OH, OH                                     5506                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      methyl       OH, OH                                     5507                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      CH.sub.2 CN  OH, OH                                     5508                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      CH.sub.2 COOH                                                                               OH, OH                                     5509                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      CH.sub.2 NC  OH, OH                                     5510                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      CH.sub.2 NO.sub.2                                                                           OH, OH                                     5511                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      (CH.sub.2).sub.2 OH                                                                         OH, OH                                     5512                                                                              CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                         H      CH.sub.2 SOCH.sub.3                                                                         OH, OH                                     5513                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      H            (+)-pin                                    5514                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      methyl       (+)-pin                                    5515                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      CH.sub.2 CN  (+)-pin                                    5516                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      CH.sub.2 COOH                                                                               (+)-pin                                    5517                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      CH.sub.2 NC  (+)-pin                                    5518                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      CH.sub.2 NO.sub.2                                                                           (+)-pin                                    5519                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      (CH.sub.2).sub.2 OH                                                                         (+)-pin                                    5520                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      CH.sub.2 SOCH.sub.3                                                                         (+)-pin                                    5521                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      H            OH, OH                                     5522                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      methyl       OH, OH                                     5523                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      CH.sub.2 CN  OH, OH                                     5524                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      CH.sub.2 COOH                                                                               OH, OH                                     5525                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      CH.sub.2 NC  OH, OH                                     5526                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      CH.sub.2 NO.sub.2                                                                           OH, OH                                     5527                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      (CH.sub.2).sub.2 OH                                                                         OH, OH                                     5528                                                                              NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                         H      CH.sub.2 SOCH.sub.3                                                                         OH, OH                                     m = 0                                                                          5529                                                                              NH(CNH)NH.sub.2                                                                         H   H      3-(t-butyl-O.sub.2 CNH)Ph                                                                   (+)-pin                                                                             BT                                    5530                                                                              NH(CNH)NH.sub.2                                                                         H   H      3-(t-butyl-O.sub.2 CNH)Ph                                                                   OH, OH                                     5531                                                                              NH(CNH)NH.sub.2                                                                         H   H      3-(NH.sub.2)Ph                                                                              (+)-pin                                    5532                                                                              NH(CNH)NH.sub.2                                                                         H   H      3-(NH.sub.2)Ph                                                                              OH, OH                                     5533                                                                              NH(CNH)NH.sub.2                                                                         H   H      3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                                    5534                                                                              NH(CNH)NH.sub.2                                                                         H   H      3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                                     5535                                                                              NH(CNH)NH.sub.2                                                                         H   H      Ph           (+)-pin                                                                             BU                                    5536                                                                              NH(CNH)NH.sub.2                                                                         H   H      Ph           OH, OH                                                                              BV                                    5537                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.3                                                                              Ph           (+)-pin                                    5538                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.3                                                                              Ph           OH, OH                                     5539                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 CN                                                                           Ph           (+)-pin                                    5540                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 CN                                                                           Ph           OH, OH                                     5541                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 COOH                                                                         Ph           (+)-pin                                    5542                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 COOH                                                                         Ph           OH, OH                                     5543                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 SO.sub.2 NH.sub.2                                                            Ph           (+)-pin                                    5544                                                                              NH(CNH)NH.sub.2                                                                         H   CH.sub.2 SO.sub.2 NH.sub.2                                                            Ph           OH, OH                                     5545                                                                              NH(CNH)NH                                                                               H   CH.sub.2 CN                                                                           3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                                    5546                                                                              NH(CNH)NH                                                                               H   CH.sub.2 CN                                                                           3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                                     5547                                                                              NH(CNH)NH                                                                               H   CH.sub.2 COOH                                                                         3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                                    5548                                                                              NH(CNH)NH                                                                               H   CH.sub.2 COOH                                                                         3-(CH.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                                     5549                                                                              NH(CNH)NH                                                                               H   CH.sub.2 COOH                                                                         2-(CH.sub.3 SO.sub.2 NH)Ph                                                                  (+)-pin                                    5550                                                                              NH(CNH)NH                                                                               H   CH.sub.2 COOH                                                                         2-(CH.sub.3 SO.sub.2 NH)Ph                                                                  OH, OH                                     5551                                                                              NH(CNH)NH.sub.2                                                                         H   H      3-(t-butylOCONH)Ph                                                                          (+)-pin                                                                             BO                                    5552                                                                              NH(CNH)NH.sub.2                                                                         H   H      Ph           (+)-pin                                                                             BQ                                    5553                                                                              NH(CNH)NH.sub.2                                                                         H   H      Ph           OH   BR                                    __________________________________________________________________________      BO. MS (M+H)+: Calc. 594, Found 594.                                           BQ. MS (M+H)+: Calc. 479, Found 479.                                           BS. MS (M+H)+: Calc. 345, Found 345.                                           BT. MS (M+H)+: Calc. 594, Found 594.                                           BU. MS (M+H)+: Calc. 479, Found 479.                                           BV. MS (M+H)+: Calc. 345, Found 345.                                     

                                      TABLE 51                                     __________________________________________________________________________      ##STR146##                                                                    Ex  X        R.sup.13                                                                            R.sup.14                                                                          R.sup.15                                                                              Y.sup.1 Y.sup.2                                                                     Phys. Data                                    __________________________________________________________________________     m = 1                                                                          5558                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  H      (+)-pin                                            5559                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  methyl (+)-pin                                            5560                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           (+)-pin                                            5561                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         (+)-pin                                            5562                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           (+)-pin                                            5563                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                            5564                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                            5565                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                            5566                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  H      OH, OH                                             5567                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  methyl OH, OH                                             5568                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           OH, OH                                             5569                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         OH, OH                                             5570                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           OH, OH                                             5571                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     OH, OH                                             5572                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                             5573                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                             5574                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  H      (+)-pin                                            5575                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  methyl (+)-pin                                            5576                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           (+)-pin                                            5577                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         (+)-pin                                            5578                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           (+)-pin                                            5579                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                            5580                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                            5581                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                            5582                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  H      OH, OH                                             5583                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  methyl OH, OH                                             5584                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           OH, OH                                             5585                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         OH, OH                                             5586                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           OH, OH                                             5587                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     OH, OH                                             5588                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                             5589                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                             m = 0                                                                          5590                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  H      (+)-pin                                            5591                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  methyl (+)-pin                                            5592                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           (+)-pin                                            5593                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         (+)-pin                                            5594                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           (+)-pin                                            5595                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                            5596                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                            5597                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                            5598                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  H      OH, OH                                             5599                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  methyl OH, OH                                             5600                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           OH, OH                                             5601                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         OH, OH                                             5602                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           OH, OH                                             5603                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     OH, OH                                             5604                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                             5605                                                                               CH.sub.2 NH.sub.2                                                                       PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                             5606                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  H      (+)-pin                                            5607                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  methyl (+)-pin                                            5608                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           (+)-pin                                            5609                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         (+)-pin                                            5610                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           (+)-pin                                            5611                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     (+)-pin                                            5612                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   (+)-pin                                            5613                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   (+)-pin                                            5614                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  H      OH, OH                                             5615                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  methyl OH, OH                                             5616                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 CN                                                                           OH, OH                                             5617                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 COOH                                                                         OH, OH                                             5618                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NC                                                                           OH, OH                                             5619                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 NO.sub.2                                                                     OH, OH                                             5620                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  (CH.sub.2).sub.2 OH                                                                   OH, OH                                             5621                                                                               NH(CNH)NH.sub.2                                                                         PhCH.sub.2                                                                          H  CH.sub.2 SOCH.sub.3                                                                   OH, OH                                             __________________________________________________________________________

                                      TABLE 52                                     __________________________________________________________________________      ##STR147##                                                                    Ex X        R.sup.13                                                                               R.sup.14                                                                               Y.sup.1 Y.sup.2                                                                     Phys. Data                                    __________________________________________________________________________     m = 0                                                                          5626                                                                              CH.sub.2 NH.sub.2                                                                       H       H       (+)-pin                                            5627                                                                              CH.sub.2 NH.sub.2                                                                       H       methyl  (+)-pin                                            5628                                                                              CH.sub.2 NH.sub.2                                                                       H       H       OH, OH                                             5629                                                                              CH.sub.2 NH.sub.2                                                                       H       methyl  OH, OH                                             5630                                                                              CH.sub.2 NH.sub.2                                                                       H       CH.sub.2 CN                                                                            (+)-pin                                            5631                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                            5632                                                                              CH.sub.2 NH.sub.2                                                                       H       CH.sub.2 CN                                                                            OH, OH                                             5633                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2).sub.2 COOH                                                                  OH, OH                                             5634                                                                              CH.sub.2 NH.sub.2                                                                       H       CH.sub.2 COOMe                                                                         (+)-pin                                            5635                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2)COOH                                                                         (+)-pin                                            5636                                                                              CH.sub.2 NH.sub.2                                                                       H       CH.sub.2 COOMe                                                                         OH, OH                                             5637                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2)COOH                                                                         OH, OH                                             5638                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2).sub.2 CN.sub.4 H                                                            (+)-pin                                            5639                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2)CN.sub.4 H                                                                   (+)-pin                                            5640                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2).sub.2 CN.sub.4 H                                                            OH, OH                                             5641                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2)CN.sub.4 H                                                                   OH, OH                                             5642                                                                              NH(CNH)NH.sub.2                                                                         H       H       (+)-pin                                            5643                                                                              NH(CNH)NH.sub.2                                                                         H       methyl  (+)-pin                                            5644                                                                              NH(CNH)NH.sub.2                                                                         H       H       OH, OH                                             5645                                                                              NH(CNH)NH.sub.2                                                                         H       methyl  OH, OH                                             5646                                                                              NH(CNH)NH.sub.2                                                                         H       CH.sub.2 CN                                                                            (+)-pin                                            5647                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                            5648                                                                              NH(CNH)NH.sub.2                                                                         H       CH.sub.2 CN                                                                            OH, OH                                             5649                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2).sub.2 COOH                                                                  OH, OH                                             5650                                                                              NH(CNH)NH.sub.2                                                                         H       CH.sub.2 COOMe                                                                         (+)-pin                                            5651                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2)COOH                                                                         (+)-pin                                            5652                                                                              NH(CNH)NH.sub.2                                                                         H       CH.sub.2 COOMe                                                                         OH, OH                                             5653                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2)COOH                                                                         OH, OH                                             5654                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2).sub.2 CN.sub.4 H                                                            (+)-pin                                            5655                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2)CN.sub.4 H                                                                   (+)-pin                                            5656                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2).sub.2 CN.sub.4 H                                                            OH, OH                                             5657                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2)CN.sub.4 H                                                                   OH, OH                                             5658                                                                              OMe      H       H       (+)-pin                                            5659                                                                              OMe      H       H       OH, OH                                             5660                                                                              NH(CNH)H H       H       (+)-pin                                            5661                                                                              NH(CNH)H H       H       OH, OH                                             5662                                                                              CH.sub.2 NH.sub.2                                                                       CH.sub.2 CN                                                                            H       (+)-pin                                            5663                                                                              CH.sub.2 NH.sub.2                                                                       CH.sub.2 CN                                                                            H       OH, OH                                             5664                                                                              NH(CNH)NH.sub.2                                                                         (CH.sub.2).sub.2 COOH                                                                  H       (+)-pin                                            5665                                                                              NH(CNH)NH.sub.2                                                                         (CH.sub.2).sub.2 COOH                                                                  H       OH, OH                                             5666                                                                              OMe      CH.sub.2 COOMe                                                                         H       (+)-pin                                            5667                                                                              OMe      CH.sub.2 COOMe                                                                         H       OH, OH                                             5668                                                                              NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H                                                            H       OH, OH                                             5669                                                                              NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H                                                            H       (+)-pin                                            m = 1                                                                          5670                                                                              CH.sub.2 NH.sub.2                                                                       H       H       (+)-pin                                            5671                                                                              CH.sub.2 NH.sub.2                                                                       H       methyl  (+)-pin                                            5672                                                                              CH.sub.2 NH.sub.2                                                                       H       H       OH, OH                                             5673                                                                              CH.sub.2 NH.sub.2                                                                       H       methyl  OH, OH                                             5674                                                                              CH.sub.2 NH.sub.2                                                                       H       CH.sub.2 CN                                                                            (+)-pin                                            5675                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                            5676                                                                              CH.sub.2 NH.sub.2                                                                       H       CH.sub.2 CN                                                                            OH, OH                                             5677                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2).sub.2 COOH                                                                  OH, OH                                             5678                                                                              CH.sub.2 NH.sub.2                                                                       H       CH.sub.2 COOMe                                                                         (+)-pin                                            5679                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2)COOH                                                                         (+)-pin                                            5680                                                                              CH.sub.2 NH.sub.2                                                                       H       CH.sub.2 COOMe                                                                         OH, OH                                             5681                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2)COOH                                                                         OH, OH                                             5682                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2).sub.2 CN.sub.4 H                                                            (+)-pin                                            5683                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2)CN.sub.4 H                                                                   (+)-pin                                            5684                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2).sub.2 CN.sub.4 H                                                            OH, OH                                             5685                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2)CN.sub.4 H                                                                   OH, OH                                             5686                                                                              NH(CNH)NH.sub.2                                                                         H       H       (+)-pin                                            5687                                                                              NH(CNH)NH.sub.2                                                                         H       methyl  (+)-pin                                            5688                                                                              NH(CNH)NH.sub.2                                                                         H       H       OH, OH                                             5689                                                                              NH(CNH)NH.sub.2                                                                         H       methyl  OH, OH                                             5690                                                                              NH(CNH)NH.sub.2                                                                         H       CH.sub.2 CN                                                                            (+)-pin                                            5691                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                            5692                                                                              NH(CNH)NH.sub.2                                                                         H       CH.sub.2 CN                                                                            OH, OH                                             5693                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2).sub.2 COOH                                                                  OH, OH                                             5694                                                                              NH(CNH)NH.sub.2                                                                         H       CH.sub.2 COOMe                                                                         (+)-pin                                            5695                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2)COOH                                                                         (+)-pin                                            5696                                                                              NH(CNH)NH.sub.2                                                                         H       CH.sub.2 COOMe                                                                         OH, OH                                             5697                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2)COOH                                                                         OH, OH                                             5698                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2).sub.2 CN.sub.4 H                                                            (+)-pin                                            5699                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2)CN.sub.4 H                                                                   (+)-pin                                            5700                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2).sub.2 CN.sub.4 H                                                            OH, OH                                             5701                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2)CN.sub.4 H                                                                   OH, OH                                             5702                                                                              OMe      H       H       (+)-pin                                            5703                                                                              OMe      H       H       OH, OH                                             5704                                                                              NH(CNH)H H       H       (+)-pin                                            5705                                                                              NH(CNH)H H       H       OH, OH                                             5706                                                                              CH.sub.2 NH.sub.2                                                                       CH.sub.2 CN                                                                            H       (+)-pin                                            5707                                                                              CH.sub.2 NH.sub.2                                                                       CH.sub.2 CN                                                                            H       OH, OH                                             5708                                                                              NH(CNH)NH.sub.2                                                                         (CH.sub.2).sub.2 COOH                                                                  H       (+)-pin                                            5709                                                                              NH(CNH)NH.sub.2                                                                         (CH.sub.2).sub.2 COOH                                                                  H       OH, OH                                             5710                                                                              OMe      CH.sub.2 COOMe                                                                         H       (+)-pin                                            5711                                                                              OMe      CH.sub.2 COOMe                                                                         H       OH, OH                                             5712                                                                              NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H                                                            H       OH, OH                                             5713                                                                              NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H                                                            H       (+)-pin                                            m = 0                                                                          5714                                                                              CH.sub.2 NH.sub.2                                                                       H       H       (+)-pin                                            5715                                                                              CH.sub.2 NH.sub.2                                                                       H       methyl  (+)-pin                                            5716                                                                              CH.sub.2 NH.sub.2                                                                       H       H       OH, OH                                             5717                                                                              CH.sub.2 NH.sub.2                                                                       H       methyl  OH, OH                                             5718                                                                              CH.sub.2 NH.sub.2                                                                       H       CH.sub.2 CN                                                                            (+)-pin                                            5719                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                            5720                                                                              CH.sub.2 NH.sub.2                                                                       H       CH.sub.2 CN                                                                            OH, OH                                             5721                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2).sub.2 COOH                                                                  OH, OH                                             5722                                                                              CH.sub.2 NH.sub.2                                                                       H       CH.sub.2 COOMe                                                                         (+)-pin                                            5723                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2)COOH                                                                         (+)-pin                                            5724                                                                              CH.sub.2 NH.sub.2                                                                       H       CH.sub.2 COOMe                                                                         OH, OH                                             5725                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2)COOH                                                                         OH, OH                                             5726                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2).sub.2 CN.sub.4 H                                                            (+)-pin                                            5727                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2)CN.sub.4 H                                                                   (+)-pin                                            5728                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2).sub.2 CN.sub.4 H                                                            OH, OH                                             5729                                                                              CH.sub.2 NH.sub.2                                                                       H       (CH.sub.2)CN.sub.4 H                                                                   OH, OH                                             5730                                                                              NH(CNH)NH.sub.2                                                                         H       H       (+)-pin                                            5731                                                                              NH(CNH)NH.sub.2                                                                         H       methyl  (+)-pin                                            5732                                                                              NH(CNH)NH.sub.2                                                                         H       H       OH, OH                                             5733                                                                              NH(CNH)NH.sub.2                                                                         H       methyl  OH, OH                                             5734                                                                              NH(CNH)NH.sub.2                                                                         H       CH.sub.2 CN                                                                            (+)-pin                                            5735                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2).sub.2 COOH                                                                  (+)-pin                                            5736                                                                              NH(CNH)NH.sub.2                                                                         H       CH.sub.2 CN                                                                            OH, OH                                             5737                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2).sub.2 COOH                                                                  OH, OH                                             5738                                                                              NH(CNH)NH.sub.2                                                                         H       CH.sub.2 COOMe                                                                         (+)-pin                                            5739                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2)COOH                                                                         (+)-pin                                            5740                                                                              NH(CNH)NH.sub.2                                                                         H       CH.sub.2 COOMe                                                                         OH, OH                                             5741                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2)COOH                                                                         OH, OH                                             5742                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2).sub.2 CN.sub.4 H                                                            (+)-pin                                            5743                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2)CN.sub.4 H                                                                   (+)-pin                                            5744                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2).sub.2 CN.sub.4 H                                                            OH, OH                                             5745                                                                              NH(CNH)NH.sub.2                                                                         H       (CH.sub.2)CN.sub.4 H                                                                   OH, OH                                             5746                                                                              OMe      H       H       (+)-pin                                            5747                                                                              OMe      H       H       OH, OH                                             5748                                                                              NH(CNH)H H       H       (+)-pin                                            5749                                                                              NH(CNH)H H       H       OH, OH                                             5750                                                                              CH.sub.2 NH.sub.2                                                                       CH.sub.2 CN                                                                            H       (+)-pin                                            5751                                                                              CH.sub.2 NH.sub.2                                                                       CH.sub.2 CN                                                                            H       OH, OH                                             5752                                                                              NH(CNH)NH.sub.2                                                                         (CH.sub.2).sub.2 COOH                                                                  H       (+)-pin                                            5753                                                                              NH(CNH)NH.sub.2                                                                         (CH.sub.2).sub.2 COOH                                                                  H       OH, OH                                             5754                                                                              OMe      CH.sub.2 COOMe                                                                         H       (+)-pin                                            5755                                                                              OMe      CH.sub.2 COOMe                                                                         H       OH, OH                                             5756                                                                              NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H                                                            H       OH, OH                                             5757                                                                              NH(CNH)H (CH.sub.2).sub.2 CN.sub.4 H                                                            H       (+)-pin                                            __________________________________________________________________________

                  TABLE 53                                                         ______________________________________                                          ##STR148##                                                                    and m = 0                                                                                                               Phys.                                 Ex   X            R.sup.13   R.sup.14                                                                            Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         5762 CH.sub.2 NH.sub.2                                                                           H          H    (+)-pin                                      5763 CH.sub.2 NH.sub.2                                                                           H          H    OH, OH                                       5764 NH(CNH)NH.sub.2                                                                             H          H    (+)-pin                                      5765 NH(CNH)NH.sub.2                                                                             H          H    OH, OH                                       5766 OMe          H          H    (+)-pin                                      5767 OMe          H          H    OH, OH                                       5768 NH(CNH)H     H          H    OH, OH                                       5769 NH(CNH)H     H          H    (+)-pin                                      5770 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    (+)-pin                                      5771 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    OH, OH                                       5772 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    (+)-pin                                      5773 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    OH, OH                                       5774 OMe          CH.sub.2 COOMe                                                                            H    (+)-pin                                      5775 OMe          CH.sub.2 COOMe                                                                            H    OH, OH                                       5776 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    OH, OH                                       5777 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    (+)-pin                                      ______________________________________                                    

                  TABLE 54                                                         ______________________________________                                          ##STR149##                                                                    and m = 0                                                                                                               Phys.                                 Ex   X            R.sup.13   R.sup.14                                                                            Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         5782 CH.sub.2 NH.sub.2                                                                           CH.sub.3   H    (+)-pin                                      5783 CH.sub.2 NH.sub.2                                                                           CH.sub.3   H    OH, OH                                       5784 NH(CNH)NH.sub.2                                                                             CH.sub.3   H    (+)-pin                                      5785 NH(CNH)NH.sub.2                                                                             CH.sub.3   H    OH, OH                                       5786 OMe          H          H    (+)-pin                                      5787 OMe          H          H    OH, OH                                       5788 NH(CNH)H     H          H    OH, OH                                       5789 NH(CNH)H     H          H    (+)-pin                                      5790 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    (+)-pin                                      5791 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    OH, OH                                       5792 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    (+)-pin                                      5793 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    OH, OH                                       5794 OMe          CH.sub.2 COOMe                                                                            H    (+)-pin                                      5795 OMe          CH.sub.2 COOMe                                                                            H    OH, OH                                       5796 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    OH, OH                                       5797 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    (+)-pin                                      ______________________________________                                    

                  TABLE 55                                                         ______________________________________                                          ##STR150##                                                                    and m = 0                                                                                                               Phys.                                 Ex   X            R.sup.13   R.sup.14                                                                            Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         5802 CH.sub.2 NH.sub.2                                                                           H          H    (+)-pin                                      5803 CH.sub.2 NH.sub.2                                                                           H          H    OH, OH                                       5804 NH(CNH)NH.sub.2                                                                             H          H    (+)-pin                                      5805 NH(CNH)NH.sub.2                                                                             H          H    OH, OH                                       5806 OMe          H          H    (+)-pin                                      5807 OMe          H          H    OH, OH                                       5808 NH(CNH)H     H          H    OH, OH                                       5809 NH(CNH)H     H          H    (+)-pin                                      5810 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    (+)-pin                                      5811 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    OH, OH                                       5812 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    (+)-pin                                      5813 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    OH, OH                                       5814 OMe          CH.sub.2 COOMe                                                                            H    (+)-pin                                      5815 OMe          CH.sub.2 COOMe                                                                            H    OH, OH                                       5816 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    OH, OH                                       5817 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    (+)-pin                                      ______________________________________                                    

                  TABLE 56                                                         ______________________________________                                          ##STR151##                                                                    and m = 0                                                                                                               Phys.                                 Ex   X            R.sup.13   R.sup.14                                                                            Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         5822 CH.sub.2 NH.sub.2                                                                           H          H    (+)-pin                                      5823 CH.sub.2 NH.sub.2                                                                           H          H    OH, OH                                       5824 NH(CNH)NH.sub.2                                                                             H          H    (+)-pin                                      5825 NH(CNH)NH.sub.2                                                                             H          H    OH, OH                                       5826 OMe          H          H    (+)-pin                                      5827 OMe          H          H    OH, OH                                       5828 NH(CNH)H     H          H    OH, OH                                       5829 NH(CNH)H     H          H    (+)-pin                                      5830 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    (+)-pin                                      5831 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    OH, OH                                       5832 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    (+)-pin                                      5833 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    OH, OH                                       5834 OMe          CH.sub.2 COOMe                                                                            H    (+)-pin                                      5835 OMe          CH.sub.2 COOMe                                                                            H    OH, OH                                       5836 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    OH, OH                                       5837 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    (+)-pin                                      ______________________________________                                    

                  TABLE 57                                                         ______________________________________                                          ##STR152##                                                                                                             Phys.                                 Ex   X            R.sup.13   R.sup.14                                                                            Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         m = 1                                                                          5842 CH.sub.2 NH.sub.2                                                                           H          H    (+)-pin                                      5843 CH.sub.2 NH.sub.2                                                                           H          H    OH, OH                                       5844 NH(CNH)NH.sub.2                                                                             H          H    (+)-pin                                      5845 NH(CNH)NH.sub.2                                                                             H          H    OH, OH                                       5846 OMe          H          H    (+)-pin                                      5847 OMe          H          H    OH, OH                                       5848 NH(CNH)H     H          H    OH, OH                                       5849 NH(CNH)H     H          H    (+)-pin                                      5850 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    (+)-pin                                      5851 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    OH, OH                                       5852 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    (+)-pin                                      5853 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    OH, OH                                       5854 OMe          CH.sub.2 COOMe                                                                            H    (+)-pin                                      5855 OMe          CH.sub.2 COOMe                                                                            H    OH, OH                                       5856 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    OH, OH                                       5857 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    (+)-pin                                      m = 0                                                                          5858 CH.sub.2 NH.sub.2                                                                           H          H    (+)-pin                                      5859 CH.sub.2 NH.sub.2                                                                           H          H    OH, OH                                       5860 NH(CNH)NH.sub.2                                                                             H          H    (+)-pin                                      5861 NH(CNH)NH.sub.2                                                                             H          H    OH, OH                                       5862 OMe          H          H    (+)-pin                                      5863 OMe          H          H    OH, OH                                       5864 NH(CNH)H     H          H    OH, OH                                       5865 NH(CNH)H     H          H    (+)-pin                                      5866 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    (+)-pin                                      5867 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    OH, OH                                       5868 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    (+)-pin                                      5869 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    OH, OH                                       5870 OMe          CH.sub.2 COOMe                                                                            H    (+)-pin                                      5871 OMe          CH.sub.2 COOMe                                                                            H    OH, OH                                       5872 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    OH, OH                                       5873 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    (+)-pin                                      ______________________________________                                    

                  TABLE 58                                                         ______________________________________                                          ##STR153##                                                                                                             Phys.                                 Ex   X            R.sup.13   R.sup.14                                                                            Y.sup.1 Y.sup.2                                                                       Data                                  ______________________________________                                         m = 1                                                                          5878 CH.sub.2 NH.sub.2                                                                           H          H    (+)-pin                                      5879 CH.sub.2 NH.sub.2                                                                           H          H    OH, OH                                       5880 NH(CNH)NH.sub.2                                                                             H          H    (+)-pin                                      5881 NH(CNH)NH.sub.2                                                                             H          H    OH, OH                                       5882 OMe          H          H    (+)-pin                                      5883 OMe          H          H    OH, OH                                       5884 NH(CNH)H     H          H    OH, OH                                       5885 NH(CNH)H     H          H    (+)-pin                                      5886 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    (+)-pin                                      5887 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    OH, OH                                       5888 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    (+)-pin                                      5889 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    OH, OH                                       5890 OMe          CH.sub.2 COOMe                                                                            H    (+)-pin                                      5891 OMe          CH.sub.2 COOMe                                                                            H    OH, OH                                       5892 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    OH, OH                                       5893 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    (+)-pin                                      m = 0                                                                          5894 CH.sub.2 NH.sub.2                                                                           H          H    (+)-pin                                      5895 CH.sub.2 NH.sub.2                                                                           H          H    OH, OH                                       5896 NH(CNH)NH.sub.2                                                                             H          H    (+)-pin                                      5897 NH(CNH)NH.sub.2                                                                             H          H    OH, OH                                       5898 OMe          H          H    (+)-pin                                      5899 OMe          H          H    OH, OH                                       5900 NH(CNH)H     H          H    OH, OH                                       5901 NH(CNH)H     H          H    (+)-pin                                      5902 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    (+)-pin                                      5903 CH.sub.2 NH.sub.2                                                                           CH.sub.2 CN                                                                               H    OH, OH                                       5904 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    (+)-pin                                      5905 NH(CNH)NH.sub.2                                                                             (CH.sub.2)COOH                                                                            H    OH, OH                                       5906 OMe          CH.sub.2 COOMe                                                                            H    (+)-pin                                      5907 OMe          CH.sub.2 COOMe                                                                            H    OH, OH                                       5908 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    OH, OH                                       5909 NH(CNH)H     (CH.sub.2)CN.sub.4 H                                                                      H    (+)-pin                                      ______________________________________                                    

                  TABLE 59                                                         ______________________________________                                          ##STR154##                                                                    Ex      X            U       Y.sup.1 Y.sup.2                                                                       Phys. Data                                 ______________________________________                                         m = 1                                                                          5914    CH.sub.2 NH.sub.2                                                                           S       (+)-pin                                           5915    NHC(NH)NH.sub.2                                                                             S       (+)-pin                                           5916    SC(NH)NH.sub.2                                                                              S       (+)-pin                                           5917    CH.sub.2 NH.sub.2                                                                           S       OH, OH                                            5918    NHC(NH)NH.sub.2                                                                             S       OH, OH                                            5919    SC(NH)NH.sub.2                                                                              S       OH, OH                                            5920    CH.sub.2 NH.sub.2                                                                           O       (+)-pin                                           5921    NHC(NH)NH.sub.2                                                                             O       (+)-pin                                           5922    SC(NH)NH.sub.2                                                                              O       (+)-pin                                           5923    CH.sub.2 NH.sub.2                                                                           O       OH, OH                                            5924    NHC(NH)NH.sub.2                                                                             O       OH, OH                                            5925    SC(NH)NH.sub.2                                                                              O       OH, OH                                            m=2                                                                            5926    CH.sub.2 NH.sub.2                                                                           S       (+)-pin                                                                               CA                                         5927    NHC(NH)NH.sub.2                                                                             S       (+)-pin                                           5928    SC(NH)NH.sub.2                                                                              S       (+)-pin                                           5929    CH.sub.2 NH.sub.2                                                                           S       OH, OH                                            5930    NHC(NH)NH.sub.2                                                                             S       OH, OH                                            5931    SC(NH)NH.sub.2                                                                              S       OH, OH                                            5932    CH.sub.2 NH.sub.2                                                                           O       (+)-pin                                           5933    NHC(NH)NH.sub.2                                                                             O       (+)-pin                                           5934    SC(NH)NH.sub.2                                                                              O       (+)-pin                                           5935    CH.sub.2 NH.sub.2                                                                           O       OH, OH                                            5936    NHC(NH)NH.sub.2                                                                             O       OH, OH                                            5937    SC(NH)NH.sub.2                                                                              O       OH, OH                                            ______________________________________                                          CA: HRMS Calc.: 543.2635, Found: 543.2643                                

                  TABLE 60                                                         ______________________________________                                          ##STR155##                                                                    Ex      X            U       Y.sup.1 Y.sup.2                                                                       Phys. Data                                 ______________________________________                                         m = 1                                                                          5942    CH.sub.2 NH.sub.2                                                                           S       (+)-pin                                           5943    NHC(NH)NH.sub.2                                                                             S       (+)-pin                                           5944    SC(NH)NH.sub.2                                                                              S       (+)-pin                                           5945    CH.sub.2 NH.sub.2                                                                           S       OH, OH                                            5946    NHC(NH)NH.sub.2                                                                             S       OH, OH                                            5947    SC(NH)NH.sub.2                                                                              S       OH, OH                                            5948    CH.sub.2 NH.sub.2                                                                           O       (+)-pin                                           5949    NHC(NH)NH.sub.2                                                                             O       (+)-pin                                           5950    SC(NH)NH.sub.2                                                                              O       (+)-pin                                           5951    CH.sub.2 NH.sub.2                                                                           O       OH, OH                                            5952    NHC(NH)NH.sub.2                                                                             O       OH, OH                                            5953    SC(NH)NH.sub.2                                                                              O       OH, OH                                            m=2                                                                            5954    CH.sub.2 NH.sub.2                                                                           S       (+)-pin                                           5955    NHC(NH)NH.sub.2                                                                             S       (+)-pin                                           5956    SC(NH)NH.sub.2                                                                              S       (+)-pin                                           5957    CH.sub.2 NH.sub.2                                                                           S       OH, OH                                            5958    NHC(NH)NH.sub.2                                                                             S       OH, OH                                            5959    SC(NH)NH.sub.2                                                                              S       OH, OH                                            5960    CH.sub.2 NH.sub.2                                                                           O       (+)-pin                                           5961    NHC(NH)NH.sub.2                                                                             O       (+)-pin                                           5962    SC(NH)NH.sub.2                                                                              O       (+)-pin                                           5963    CH.sub.2 NH.sub.2                                                                           O       OH, OH                                            5964    NHC(NH)NH.sub.2                                                                             O       OH, OH                                            5965    SC(NH)NH.sub.2                                                                              O       OH, OH                                            ______________________________________                                    

                                      TABLE 61                                     __________________________________________________________________________      ##STR156##                                                                    Ex  X       R.sup.A                                                                            R.sup.C                                                                               R.sup.D                                                                             Y.sup.1,Y.sup.2                                                                     Phys Data                                     __________________________________________________________________________     5970                                                                               NHC(NH)NH.sub.2                                                                        Me  Ph     OMe  (+)-pin                                            5971                                                                               NHC(NH)NH.sub.2                                                                        Me  Ph     CONH.sub.2                                                                          (+)-pin                                            5972                                                                               NHC(NH)NH.sub.2                                                                        Me  Ph     F    (+)-pin                                            5973                                                                               NHC(NH)NH.sub.2                                                                        Me  Ph     CF.sub.3                                                                            (+)-pin                                            5974                                                                               NHC(NH)NH.sub.2                                                                        Me  Ph     Cl   (+)-pin                                            5975                                                                               NHC(NH)NH.sub.2                                                                        Me  Ph     OH   (+)-pin                                            5976                                                                               NHC(NH)NH.sub.2                                                                        Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          OMe  (+)-pin                                            5977                                                                               NHC(NH)NH.sub.2                                                                        Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          CONH.sub.2                                                                          (+)-pin                                            5978                                                                               NHC(NH)NH.sub.2                                                                        Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          F    (+)-pin                                            5979                                                                               NHC(NH)NH.sub.2                                                                        Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          CF.sub.3                                                                            (+)-pin                                            5980                                                                               NHC(NH)NH.sub.2                                                                        Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          Cl   (+)-pin                                            5981                                                                               NHC(NH)NH.sub.2                                                                        Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          OH   (+)-pin                                            5982                                                                               SC(NH)NH.sub.2                                                                         Me  Ph     OMe  (+)-pin                                            5983                                                                               SC(NH)NH.sub.2                                                                         Me  Ph     CONH.sub.2                                                                          (+)-pin                                            5984                                                                               SC(NH)NH.sub.2                                                                         Me  Ph     F    (+)-pin                                            5985                                                                               SC(NH)NH.sub.2                                                                         Me  Ph     CF.sub.3                                                                            (+)-pin                                            5986                                                                               SC(NH)NH.sub.2                                                                         Me  Ph     Cl   (+)-pin                                            5987                                                                               SC(NH)NH.sub.2                                                                         Me  Ph     OH   (+)-pin                                            5988                                                                               SC(NH)NH.sub.2                                                                         Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          OMe  (+)-pin                                            5989                                                                               SC(NH)NH.sub.2                                                                         Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          CONH.sub.2                                                                          (+)-pin                                            5990                                                                               SC(NH)NH.sub.2                                                                         Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          F    (+)-pin                                            5991                                                                               SC(NH)NH.sub.2                                                                         Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          CF.sub.3                                                                            (+)-pin                                            5992                                                                               SC(NH)NH.sub.2                                                                         Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          Cl   (+)-pin                                            5993                                                                               SC(NH)NH.sub.2                                                                         Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          OH   (+)-pin                                            5994                                                                               CH.sub.2 NH.sub.2                                                                      Me  Ph     OMe  (+)-pin                                            5995                                                                               CH.sub.2 NH.sub.2                                                                      Me  Ph     CONH.sub.2                                                                          (+)-pin                                            5996                                                                               CH.sub.2 NH.sub.2                                                                      Me  Ph     F    (+)-pin                                            5997                                                                               CH.sub.2 NH.sub.2                                                                      Me  Ph     CF.sub.3                                                                            (+)-pin                                            5998                                                                               CH.sub.2 NH.sub.2                                                                      Me  Ph     Cl   (+)-pin                                            5999                                                                               CH.sub.2 NH.sub.2                                                                      Me  Ph     OH   (+)-pin                                            6000                                                                               CH.sub.2 NH.sub.2                                                                      Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          OMe  (+)-pin                                            6001                                                                               CH.sub.2 NH.sub.2                                                                      Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          CONH.sub.2                                                                          (+)-pin                                            6002                                                                               CH.sub.2 NH.sub.2                                                                      Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          F    (+)-pin                                            6003                                                                               CH.sub.2 NH.sub.2                                                                      Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          CF.sub.3                                                                            (+)-pin                                            6004                                                                               CH.sub.2 NH.sub.2                                                                      Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          Cl   (+)-pin                                            6005                                                                               CH.sub.2 NH.sub.2                                                                      Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          OH   (+)-pin                                            6006                                                                               NHC(NH)NH.sub.2                                                                        Me  Ph     OMe  OH, OH                                             6007                                                                               NHC(NH)NH.sub.2                                                                        Me  Ph     CONH.sub.2                                                                          OH, OH                                             6008                                                                               NHC(NH)NH.sub.2                                                                        Me  Ph     F    OH, OH                                             6009                                                                               NHC(NH)NH.sub.2                                                                        Me  Ph     CF.sub.3                                                                            OH, OH                                             6010                                                                               NHC(NH)NH.sub.2                                                                        Me  Ph     Cl   OH, OH                                             6011                                                                               NHC(NH)NH.sub.2                                                                        Me  Ph     OH   OH, OH                                             6012                                                                               NHC(NH)NH.sub.2                                                                        Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          OMe  OH, OH                                             6013                                                                               NHC(NH)NH.sub.2                                                                        Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          CONH.sub.2                                                                          OH, OH                                             6014                                                                               NHC(NH)NH.sub.2                                                                        Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          F    OH, OH                                             6015                                                                               NHC(NH)NH.sub.2                                                                        Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          CF.sub.3                                                                            OH, OH                                             6016                                                                               NHC(NH)NH.sub.2                                                                        Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          Cl   OH, OH                                             6017                                                                               NHC(NH)NH.sub.2                                                                        Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          OH   OH, OH                                             6018                                                                               SC(NH)NH.sub.2                                                                         Me  Ph     OMe  OH, OH                                             6019                                                                               SC(NH)NH.sub.2                                                                         Me  Ph     CONH.sub.2                                                                          OH, OH                                             6020                                                                               SC(NH)NH.sub.2                                                                         Me  Ph     F    OH, OH                                             6021                                                                               SC(NH)NH.sub.2                                                                         Me  Ph     CF.sub.3                                                                            OH, OH                                             6022                                                                               SC(NH)NH.sub.2                                                                         Me  Ph     Cl   OH, OH                                             6023                                                                               SC(NH)NH.sub.2                                                                         Me  Ph     OH   OH, OH                                             6024                                                                               SC(NH)NH.sub.2                                                                         Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          OMe  OH, OH                                             6025                                                                               SC(NH)NH.sub.2                                                                         Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          CONH.sub.2                                                                          OH, OH                                             6026                                                                               SC(NH)NH.sub.2                                                                         Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          F    OH, OH                                             6027                                                                               SC(NH)NH.sub.2                                                                         Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          CF.sub.3                                                                            OH, OH                                             6028                                                                               SC(NH)NH.sub.2                                                                         Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          Cl   OH, OH                                             6029                                                                               SC(NH)NH.sub.2                                                                         Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          OH   OH, OH                                             6030                                                                               CH.sub.2 NH.sub.2                                                                      Me  Ph     OMe  OH, OH                                             6031                                                                               CH.sub.2 NH.sub.2                                                                      Me  Ph     CONH.sub.2                                                                          OH, OH                                             6032                                                                               CH.sub.2 NH.sub.2                                                                      Me  Ph     F    OH, OH                                             6033                                                                               CH.sub.2 NH.sub.2                                                                      Me  Ph     CF.sub.3                                                                            OH, OH                                             6034                                                                               CH.sub.2 NH.sub.2                                                                      Me  Ph     Cl   OH, OH                                             6035                                                                               CH.sub.2 NH.sub.2                                                                      Me  Ph     OH   OH, OH                                             6036                                                                               CH.sub.2 NH.sub.2                                                                      Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          OMe  OH, OH                                             6037                                                                               CH.sub.2 NH.sub.2                                                                      Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          CONH.sub.2                                                                          OH, OH                                             6038                                                                               CH.sub.2 NH.sub.2                                                                      Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          F    OH, OH                                             6039                                                                               CH.sub.2 NH.sub.2                                                                      Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          CF.sub.3                                                                            OH, OH                                             6040                                                                               CH.sub.2 NH.sub.2                                                                      Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          Cl   OH, OH                                             6041                                                                               CH.sub.2 NH.sub.2                                                                      Me  4-C.sub.6 H.sub.4 CO.sub.2 H                                                          OH   OH, OH                                             __________________________________________________________________________

Utility

The compounds of formula (I) are useful as inhibitors of trypsin-like enzymes, notably human thrombin, Factor VIIa, Factor IXa, Factor Xa, plasma kallikrein and plasmin. Because of their inhibitory action, these compounds are indicated for use in the prevention or treatment of physiological reactions catalyzed by the aforesaid enzymes such as blood coagulation and inflammation. These compounds are also useful as anticoagulants for the processing of blood for therapeutic or diagnostic purposes or for the production of blood products or fragments, since contact of blood with the surfaces commonly used for blood collection and storage causes activation of coagulation leading to thrombin formation and clot formation.

The effectiveness of compounds of the present invention as inhibitors of blood coagulation proteases was determined using purified human proteases and synthetic substrates following procedures similar to those described in Kettner et al. (1990).

For these assays, the rate of enzymatic (thrombin, Factor Xa, and Factor VIIa) hydrolysis of chromogenic substrates (S2238 (H-D-Phe-Pip-Arg-pNA), S2222, and S2288, respectively; Kabi Pharmacia, Franklin, Ohio) was measured both in the absence and presence of compounds of the present invention. Hydrolysis of the substrate resulted in the release of pNA, which was monitored spectrophotometrically by measuring the increase in absorbance at 405 nM. A decrease in the rate of absorbance change at 405 nm in the presence of inhibitor is indicative of enzyme inhibition. The results of this assay are expressed as inhibitory constant, K_(i).

Thrombin and Xa determinations were made in 0.10M sodium phosphate buffer, pH 7.5, containing 0.20M NaCl, and 0.5% PEG 8000. VIIa determinations were made in 0.05M tris buffer, pH 7.6, containing 0.10M NaCl, 4 mM CaCl₂, and 0.1% bovine serum albumin. The Michaelis constant, K_(m), for substrate hydrolysis was determined at 25° C. using the method of Lineweaver and Burk.

Values of K_(i) were determined by allowing 0.2-0.5 nM human thrombin or human factor Xa (Enzyme Research Laboratories, South Bend, Ind.), or 50 nM human factor VIIa (BiosPacific, Emeryville, Calif.) react with the substrate (0.20 mM-1 mM) in the presence of inhibitor. Reactions were allowed to go for 30 minutes and the velocities (rate of absorbance change vs time) were measured in the time frame of 25-30 minutes. The following relationship was used to calculate K_(i) values. ##EQU1## where: v_(o) is the velocity of the control in the absence of inhibitor;

v_(s) is the velocity in the presence of inhibitor;

I is the concentration of inhibitor;

K_(i) is the dissociation constant of the enzyme: inhibitor complex;

S is the concentration of substrate;

K_(m) is the Michaelis constant.

Using the methodology described above, representative compounds of this invention were evaluated and found to exhibit a K_(i) of less 500 μM thereby confirming the utility of compounds of the invention as effective inhibitors of human blood coagulation proteases. The results of these assays are summarized in Table 62, where +++ indicates a K_(i) <500 nM; ++ indicates a K_(i) <50,000 nM; and + indicates a K_(i) 500,000<nM; - indicates inactive.

Table 62

K_(i) values for inhibition of Serine Proteases by compounds of the present invention.

    ______________________________________                                         EXAMPLE    Thrombin   Factor Xa Factor VIIa                                    ______________________________________                                           1        +++        ++        NT                                               2        +++        +++       +++                                             29        +++        NT        NT                                              35        +++        +++       ++                                              68        ++         ++        +++                                             129       +++        +++       NT                                              199       +++        +++       +++                                             203       +++        +++       +++                                             224       +++        +++       +++                                             227       +++        +++       ++                                              231       +++        +++       ++                                              261       +++        +++       +++                                             262       +++        +++       +++                                             263       +++        +++       +++                                             283       +++        +++       ++                                              286       +++        +++       +++                                             288       +++        NT        +++                                             298       +++        +++       +++                                             299       +++        +++       +++                                             302       +++        +++       ++                                              303       +++        ++        ++                                              304       ++         ++        ++                                              305       ++         ++        ++                                              468       ++         ++        ++                                              474       ++         ++        ++                                              887       +++        NT        NT                                              888       +++        ++        ++                                              890       +++        ++        ++                                              892       +++        ++        ++                                              898       +++        ++        ++                                              905       ++         ++        -                                               913       +++        -         ++                                              914       +++        ++        ++                                              917       +++        ++        ++                                              920       +++        NT        NT                                              921       +++        ++        ++                                              923       +++        ++        ++                                              931       +++        ++        ++                                              967       +++        ++        +++                                             969       +++        ++        ++                                              977       +++        NT        NT                                             1352       +++        ++        NT                                             1431       +++        NT        NT                                             1459       ++         ++        ++                                             1467       +++        NT        ++                                             1521       +++        NT        NT                                             1557       +++        NT        ++                                             2066       NT         NT        NT                                             2067       +++        NT        NT                                             2068       ++         ++        ++                                             2073       +++        ++        ++                                             2074       +++        ++        ++                                             2411       +++        NT        NT                                             2412       +++        ++        ++                                             2414       +++        ++        ++                                             2416       +++        ++        ++                                             2422       +++        ++        ++                                             2430       ++         ++        -                                              2439       +++        ++        ++                                             2440       +++        ++        ++                                             2443       +++        ++        ++                                             2446       +++        ++        ++                                             2447       +++        ++        ++                                             2490       +++        ++        +++                                            2491       +++        +++       ++                                             2499       +++        ++        ++                                             2533       +++        ++        --                                             2752       +++        NT        NT                                             2780       +++        ++        +++                                            2781       +++        ++        ++                                             2837       ++         NT        NT                                             3349       +++        ++        NT                                             3458       +++        -         ++                                             3465       +++        ++        ++                                             3538       +++        ++        ++                                             4064       ++         ++        ++                                             4065       ++         ++        ++                                             5426       +++        +++       NT                                             5529       +++        +++       NT                                             5551       NT         NT        NT                                             ______________________________________                                    

The final concentration of thrombin was 4 NIH units/mL. The effectiveness of compounds in prolonging clotting times is reported as K_(i) TT (nM; level of inhibitor required to prolong clotting to the time observed for 2 NIH units/mL thrombin in the absence of inhibitor). Compounds of the present invention were found to have K_(i) TT values in the range of 100-6000 nm.

Generally, these compounds may be administered orally or parenterally to a host to obtain an anti-thrombogenic effect. The dosage of the active compound depends on the mammalian species, body weight, age, and mode of administration as will be obvious to one skilled in the art. In the case of large mammals such as humans, the compounds may be administered alone or in combination with pharmaceutical carriers or diluents at a dose of from 0.02 to 15 mg/Kg to obtain the anti-thrombogenic effect, and may be given as a single dose or in divided doses or as a sustained release formulation.

Pharmaceutical carriers or diluents are well known and include sugars, starches and water, which may be used to make tablets, capsules, injectable solutions or the like which can serve as suitable dosage forms for administration of the compounds of this invention. Remington's Pharmaceutical Sciences, A. Osol, is a standard reference text which discloses suitable pharmaceutical carriers and dosage forms. The disclosure of this text is hereby incorporated by reference for a more complete teaching of suitable dosage forms for administration of the compounds of this invention. 

What is claimed is:
 1. A compound of formula:

    R.sup.1 --Z--CHR.sup.2 --A                                 (I)

wherein: A is--BY¹ Y², Y¹ and Y² are independently--OH; Y¹ and Y² can be taken together to form:a) a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms and, from 0-3 heteroatoms which can be N, S, or O, b) a cyclic boron amide where said chain or ring contains from 2 to 20 carbon atoms and,from 0-3 heteroatoms which can be N, S, or O, c) a cyclic boron amide-ester where said chain or ring contains from 2 to 20 carbon atoms and from 0-3 heteroatoms which can be N, S, or O; Z isa)--(CH₂)_(m) CONR⁸ --, b)--(CH₂)_(m) CSNR⁸ --, c)--(CH₂)_(m) SO₂ NR⁸ --, d)--(CH₂)_(m) CO₂ --, e)--(CH₂)_(m) C(S)O--, or f)--(CH₂)_(m) SO₂ O--; R¹ isa) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted:i) quinolinyl, ii) isoquinolinyl, iii) benzopyranyl, iv) benzothiophenyl, v) benzofuranyl, vi) 5,6,7,8-tetrahydroquinolinyl, vii) 5,6,7,8-tetrahydroisoquinolinyl, and wherein the substituents are members selected from the group consisting of halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, R⁸, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONHR⁸, NR⁸ COR⁹, NR⁸ CO₂ R⁹, ##STR157## wherein J is N or C and K, L, M and Q are independently selected at each occurrence from the group consisting of N, CR¹³, S or O, provided that:i) there may be only one S or O present in the ring at a time; ii) there may only be 1-2N present when there is an O or S present; iii) there may be only 1-4N present; ##STR158## wherein W, R, T, U and V are selected from the group consisting of: CR¹³ or N, provided that there be no less than 1 and no more than 3N present; ##STR159## is as defined above; ##STR160## is as defined above; ##STR161## wherein G is O, S, or NP, where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³); ##STR162## wherein G is O, S, or NP, where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³); R² isa) --(C1-C12 alkyl)--X, b) --(C2-C12 alkenyl)--X, or ##STR163## X is a) halogen (F, Cl, Br, I), b) --CN, c) --NO₂, d) --CF₃, e) --S(O)_(r) R¹⁴, f) --NHR¹⁴ g) --NHS(O)_(r) R¹⁴, h) --NHC(NH)H, i) --NHC(NH)NHOH, j) --NHC(NH)NHCN, k) --NHC(NH)NHR¹⁴, l) --NHC(NH)NHCOR¹⁴, m) --C(NH)NHR¹⁴, n) --C(NH)NHCOR¹⁴, o) --C(O)NHR¹⁴, p) --C(O)NHC(O)R¹⁴, q) --C(O)OR¹⁴, r) --OR¹⁴, s) --OC(O)R¹⁴, t) --OC(O)OR¹⁴, u) --OC(O)NHR¹⁴, v) --OC(O)NHC(O)R¹⁴, w) --SC(═NH)NHR¹⁴, or x) --SC(═NH)NHC(═O)R¹⁴ ; R³ isa) hydrogen, b) C₁ -C₈ alkyl, c) --(C₁ -C₄ alkyl)-aryl, d) C₅ -C₇ cycloalkyl, or e) phenyl; R⁵ and R⁶ are hydrogen or when taken together form a six membered aromatic ring optionally substituted with one, two or three substituents selected from the group consisting of halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONR⁸ R⁹, phenyl, benzyl, phenylethyl; R⁷ isa) phenyl, b) C₁ -C₈ -alkyl, c) C₁ -C₄ -alkoxy, d) --CF₃, or e) benzyl; R⁸ and R⁹ are independentlya) H, ##STR164## c) C₃ -C₇ cycloalkyl, d) C₁ -C₈ -alkyl, or R¹¹ isa) halo (F, Cl, Br, I), b) --CN, c) C₁ -C₁₀ -alkyl, d) C₃ -C₈ -cycloalkyl, e) C₂ -C₁₀ -alkenyl, f) C₂ -C₁₀ -alkynyl, g) --OR⁸, h) --NO₂, i) --CF₃, j) --S(O)_(r) R⁷, k) --NR⁸ R⁹, m) --CO₂ R⁸, l) --COR⁹, n) --CONR⁸ R⁹, or o) H R¹² isH, C₁ -C₄ alkyl, phenyl, benzyl, --COR⁷, or --S(O)_(r) R⁷ ; R¹³ isH, halogen (F, Cl, Br, I), (C₁ -C₈)alkyl, (C₁ -C₆)-perfluoroalkyl, --(CH₂)_(r) -D, C₃ -C₈ cycloalkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, methylenedioxy, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) NC, --(CH₂)_(w) CN, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ -(C₁ -C₆)alkyl, --(CH₂)_(w) SO₂ NH, --(CH₂)_(w) NHSO₂ --(CH₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(C═O)--(C₁ -C₅ alkyl), --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO-(phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO₂ -(phenyl), --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, --S--(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, or --O--(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸ ; R¹⁴ isa) --H, b) --CF₃ c) --C₁ -C₄ alkyl, d) --(CH₂)_(q) -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl unsubstituted or substituted with one to three substituents selected from the group consisting of:halogen (F, Cl, Br, I), --CF₃, --(C₁ -C₄ alkyl), --(CH₂)_(x) R¹⁵, --(CH₂)_(x) CO(CH₂)_(y) R¹⁵, --(CH₂)_(x) C(O)O(CH₂)_(y) R¹⁵, --(CH₂)_(x) C(O)N[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ], --methylenedioxy, --(C₁ -C₄ alkoxy), --(CH₂)_(x) O(CH₂)_(y) R¹⁵, --(CH₂)_(x) OCO(CH₂)_(y) R¹⁵, --(CH₂)_(x) OC(O)O(CH₂)_(y) R¹⁵, --(C₂)_(x) OC(O)N[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ], --(CH₂)_(x) OC(O)N[(CH₂)_(y) R¹⁵ ] [CO(CH₂)_(y) R¹⁶ ], --(CH₂)_(x) S(O)_(r) (CH₂)y^(R) 15, --(CH₂)_(x) S(O)_(r) (CH₂)_(y) COR¹⁵, --(CH₂)_(x) S(O)_(r) (CH₂)_(y) C(O)OR¹⁵, --(CH₂)_(x) S(O)_(r) N[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ] --(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ], --(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ] [CO(CH₂)_(y) R¹⁶ ], --(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ] [C(O)O(CH₂)_(y) R¹⁶ ], --(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ] CON[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ], --(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ]CON[(CH₂)_(y) R¹⁵ ]--[CO(CH₂)_(y) R¹⁶ ], (CH₂)_(x) N[(CH₂)_(y) R¹⁵ ] [S(O)_(r) (CH₂)_(y) R¹⁶ ]; R¹⁵ and R¹⁶ are independentlya) hydrogen, b) --(C₁ -C₈ alkyl, c) --(C₁ -C₄ alkyl)-aryl, where aryl is defined above,d) C₅ -C₇ cydoalkyl, e) phenyl, substituted by 0-3 R¹⁸, f) benzyl, substituted by 0-3 R¹⁸, or g) --(C₁ -C₄ alkoxy); R¹⁵ and R¹⁶ can be taken together to form a ring: ##STR165## R¹⁸ and R¹⁹ are independently H, halo (F, Cl, Br, I), C₁ -C₈ -alkyl, C₃ -C₈ cycloalkyl, C₂ -C₆ -alkenyl, C₂ -C₆ -alkynyl, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) CF₃, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --CH₂)_(w) SO₂ NH--(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ -(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ (C₁ -C₆ -phenyl), or --O(C═O)phenyl; R18 and R19 can be taken together to form a methylenedioxy group; R²⁰ and R^(20a) are independently:(C₁ -C₈)alkyl, --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, (C₁ -C₆)-perfluoroalkyl,or --(CH₂)_(r) --D; m is 0 to 6; n is 1 to 2; p is 0 to 2; q is 0 to
 4. r is 0 to 2; s is 0 to 3; t is 1 to 5; u is 0 to 5; w is 0 to 5; x is 0 to 6; y is 0 to 6; D is fur-2-yl, fur-3-yl, thiophen-2-yl, thiophen-3-yl, oxazol-2-yl, oxazol-4-yl, thiazol-2-yl, thiazol-4-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, pyrid-2-yl, pyrid-4-yl, pyridazin-3-yl, pyridazin-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrazin-2-yl, or tetrazoly; E is --CO--, --SO₂ --, --CH₂ -- or a single bond, F is --CO--; W isa) --O--, b) --S(O)_(r) --, c) --NR⁴ --, d) --NC(═O)R³ --, e) a bond, or f) --(CH₂)_(n) --;or pharmaceutically acceptable salts thereof.
 2. A compound of claim 1 wherein:Z isa) --(CH₂)_(m) CONR⁸ --, b) --(CH₂)_(m) CSNR⁸ --, c) --(CH₂)_(m) SO₂ NR⁸ --, R¹ isa) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted:i) quinolinyl, ii) isoquinolinyl, iii) benzopyranyl, iv) benzothiophenyl, v) benzofuranyl, vi) 5,6,7,8-tetrahydroquinolinyl, vii) 5,6,7,8-tetrahydroisoquinolinyl, and wherein the substituents are selected from the group consisting of halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, R⁸, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONR⁸ H, NR⁸ COR⁹, NR⁸ CO₂ R⁹ ; ##STR166## e) wherein the ring ##STR167## represented by --J--K--L--M--Q-- is a group selected from: 1) --N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,2) --N--C(R¹³)═C(R¹³)--C(R¹³)═N--, 3) --N--C(R¹³)═C(R¹³)--N═C(R¹³)--, 4) --N--C(R¹³)═N--C(R¹³)═N--, 5) --N--C(R¹³)═C(R¹³)--N═N-- 6) --N--C(R¹³)═N--N═N--, 7) --N--N═C(R¹³)--N═N--, 8) ═C--O--C(R¹³)═N--C(R¹³)═, 9) --C═C(R¹³)--O--C(R¹³)═N--, 10) ═C--O--C(R¹³)═C(R¹³)--N═, 11) --C═C(R¹³)--C(R¹³)═N--O--, 12) ═C--C(R¹³)═C(R¹³)--O--N═, 13) --C═C(R¹³)--O--N═C(R¹³)--, 14) ═C--S--C(R¹³)═N--C(R¹³)═, 15) --C═C(R¹³)--S--C(R¹³)═N--, 16) ═C--S--C(R¹³)═C(R¹³)--N═, 17) --C═N--S--N═C(R¹³)--, 18) --C═N--S--C(R¹³)═N--, 19) ═C--S--N═C(R¹³)--N═, 20) ═C--S--C(R¹³)═C(R¹³)--C(R¹³)═, 21) --C═C(R¹³)--S--C(R¹³)═C(R¹³)--, 22) --C--O--C(R¹³)═C(R¹³)--C(R¹³)═, or 23) --C═C(R¹³)--O--C(R¹³)═C(R¹³)--; f) wherein the ring ##STR168## represented by --C--W--R--T--U--V-- is a group selected from: 1) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--,2) --C═C(R¹³)--N═C(R¹³)--C(R¹³)═C(R¹³)--, 3) --C═C(R¹³)--C(R¹³)═N--C(R¹³)═C(R¹³)--, 4) --C═N--N═C(R¹³)--C(R¹³)═C(R¹³)--, 5) --C═C(R¹³)--N═N--C(R¹³)═C(R¹³)--, 6) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═N--, 7) --C═N--C(R¹³)═C(R¹³)--N═C(R¹³)--, 8) --C═N--C(R¹³)═N--C(R¹³)═C(R¹³)--, 9) --C═C(R¹³)--N═C(R¹³)--N═C(R¹³)--, 10) --C═N--C(R¹³)═N--N═C(R¹³)--, 11) --C═N--(R¹³)═C(R¹³)--N═N--, or 12) --C═C(R¹³)--N═C(R¹³)--N═N--; ##STR169## is as defined above; ##STR170## is as defined above; ##STR171## wherein G is O, S, or NP (where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³ ; ##STR172## wherein G is O, S, or NP (where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³ ; R¹⁴ is:a) --H, b) --CF₃ c) --C₁ -C₄ alkyl, d) --(CH₂)_(q) -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl unsubstituted or substituted with one to three substituents selected from the group consisting of:halogen (F, Cl, Br, I), --CF₃, --(C₁ -C₄ alkyl), --methylenedioxy, --(C₁ -C₄ alkoxy), --(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ];and all other required substituents of formula (I) are defined in claim
 1. 3. A compound of claim 2 whereinZ isa) --(CH₂)_(m) CONR⁸ --, b) --(CH₂)_(m) CSNR⁸ --, or c) --(CH₂)_(m) SO₂ NR⁸ --; R¹ isa) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted:i) quinolinyl, ii) isoquinolinyl, iii) benzopyranyl, iv) benzothiophenyl, v) benzofuranyl, vi) 5,6,7,8-tetrahydroquinolinyl, vii) 5,6,7,8-tetrahydroisoquinolinyl, wherein the substituents are members selected from the group consisting of: halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, R⁸, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONR⁸ H, NR⁸ COR⁹, NR⁸ CO₂ R⁹ ; ##STR173## wherein the ring represented by --J--K--L--M--Q-- is a group selected from:1) --N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--, 2) --N--C(R¹³)═C(R¹³)--C(R¹³)═N--, 3) --N--C(R¹³)═C(R¹³)--N═C(R¹³)--, 4) --N--C(R¹³)═N--C(R¹³)═N--, 5) --N--C(R¹³)═C(R¹³)--N═N-- 6) --N--C(R¹³)═N--N═N--, 7) --N--N═C(R¹³)--N═N--, 8) ═C--O--C(R¹³)═N--C(R¹³)═, 9) --C═C(R¹³)--O--C(R¹³)═N--, 10) ═C--O--C(R¹³)═C(R¹³)--N═, 11) --C═C(R¹³)--C(R¹³)═N--O--, 12) ═C--C(R¹³)═C(R¹³)--O--N═, 13) --C═C(R¹³)--O--N═C(R¹³)--, 14) ═C--S--C(R¹³)═N--C(R¹³)═, 15) --C═C(R¹³)--S--C(R¹³)═N--, 16) ═C--S--C(R¹³)═C(R¹³)--N═, 17) ═C--S--C(R¹³)═C(R¹³)--C(R¹³)═, 18) --C═C(R¹³)--S--C(R¹³)═C(R¹³)--, 19) ═C--O--C(R¹³)═C(R¹³)--C(R¹³)═, or 20) --C═C(R¹³)--O--C(R¹³)═C(R¹³)--; ##STR174## wherein the ring represented by --C--W--R--T--U--V-- is a group selected from: 1) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)--, 2) --C═C(R¹³)--N═C(R¹³)--C(R¹³)═C(R¹³)--, 3) --C═C(R¹³)--C(R¹³)═N--C(R¹³)═C(R¹³)--, 4) --C═N--N═C(R¹³)--C(R¹³)═C(R¹³)--, 5) --C═C(R¹³)--N═N--C(R¹³)═C(R¹³)--, 6) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═N--, 7) --C═N--C(R¹³)═C(R¹³)--N═C(R¹³)--, 8) --C═N--C(R¹³)═N--C(R¹³)═C(R¹³)--, 9) --C═C(R¹³)--N═C(R¹³)--N═C(R¹³)--, 10) --C═N--C(R¹³)═N--N═C(R¹³)--, 11) --C═N--C(R¹³)═C(R¹³)--N═N--, or 12) --C═C(R¹³)--N═C(R¹³)--N═N--; ##STR175## is as defined above; ##STR176## is as defined above; or ##STR177## wherein G is O, S, or NP (where P is an amine protecting group selected from the group consisting of: --R³, --C(═O)R³, --SO₂ R³, --C(═O)OR³); R² isa) --(C₁ -C₁₂ alkyl)--X,b) --(C₂ -C₁₂ alkenyl)--X, or ##STR178## X is a) halogen (F, Cl, Br, I), b) --CN, c) --NO₂, d) --CF₃, e) --NHR¹⁴ f) --NHS(O)_(r) ^(R) 14, --NHC(NH)H, h) --NHC(NH)NHOH, i) --NHC(NH)NHCN, j) --NHC(NH)NHR¹⁴, k) --NHC(NH)NHCOR¹⁴, l) --C(NH)NHR¹⁴, m) --C(NH)NHCOR¹⁴, n) --C(O)NHR¹⁴, o) --C(O)NHC(O)R¹⁴, p) --C(O)OR¹⁴, q) --OR¹⁴, r) --OC(O)R¹⁴, s) --OC(O)OR¹⁴, t) --OC(O)NHR¹⁴, u) --OC(O)NHC(O)R¹⁴, v) --SC(═NH)NHR¹⁴, or w) --SC(═NH)NHC(═O)R¹⁴ ; R¹³ isH, halogen (F, Cl, Br, I), (C₁ -C₆)alkyl, --(CH₂)_(r) --D, methylenedioxy, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) NC, --(CH₂)_(w) CN, --(CH₂)_(w) NO₂, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ 1∝C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(w) CN, --NH(CH₂)_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ (C₁ -C₆ phenyl), --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, or --O(C═O)phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸ ; R¹⁴ isa) --H, b) --CF₃ c) --C₁ -C₄ alkyl, d)--(CH₂)_(q) -aryl, wherein aryl is phenyl, biphenyl, naphthyl, or fluorenyl unsubstituted or substituted with one to three substituents selected from the group consisting of:halogen (F, Cl, Br, I), --CF₃, --(C₁ -C₄ alkyl), --methylenedioxy, --(C₁ -C₄ alkoxy), or --(CH₂)_(x) N[(CH₂)_(y) R¹⁵ ] [(CH₂)_(y) R¹⁶ ]; R¹⁸ and R¹⁹ are independentlyH, halo (F, Cl, Br, I), C₁ -C₆ -alkyl, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl,--(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(w) CN, --NH(CH₂ )_(w) CN, --S(CH₂)_(w) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) --NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -phenyl), or --O(C═O)phenyl; R18 and R19 can be taken together to form a methylenedioxy group; R²⁰ and R^(20a) are independently(C₁ -C₈)alkyl, --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸, (C₁ -C₆)-perfluoroalkyl,or --(CH₂)_(r) --D; D is fur-2-yl, fur-3-yl, thiophen-2-yl, thiophen-3-yl, oxazol-2-yl, oxazol-4-yl, thiazol-2-yl, thiazol-4-yl, pyrid-2-yl, pyrid-4-yl, pyrimidin-2-yl, or pyrimidin-4-yl;and all other required substituents of formula (I) are as in claim
 2. 4. A compound of claim 3 wherein:Z is --(CH₂)_(m) CONR⁸ --; R¹ isa) heteroaryl, wherein heteroaryl is an unsubstituted, monosubstituted or disubstituted isoquinolinyl wherein the substituents are members selected from the group consisting of: halo (F, Cl, Br, I), --CN, C₁ -C₁₀ -alkyl, C₃ -C₈ -cycloalkyl, C₂ -C₁₀ -alkenyl, C₂ -C₁₀ -alkynyl, R⁸, --OR⁸, --NO₂, --CF₃, --S(O)_(r) R⁷, --NR⁸ R⁹, --COR⁸, --CO₂ R⁸, --CONR⁸ R⁹, NR⁸ CO₂ R⁹, ##STR179## wherein the ring represented by --J--K--L--M--Q-- is a group selected from:1) --N--C(R¹³)═N--C(R¹³)═N--, 2) --N--C(R¹³)═C(R¹³)--N═N--, 3) --N--N═C(R¹³)--N═N--, 5) --N--C(R¹³)═N--N═N--, 6) --C--S--C(R¹³)═C(R¹³)--C(R¹³)═, or 7) ═C--O--C(R¹³)═C(R¹³)--C(R¹³)═; ##STR180## wherein the ring represented by --C--W--R--T--U--V-- is a group selected from: 1) --C═N--C(R¹³)═C(R¹³)═C(R¹³)--C(R¹³)═C(R¹³)-- 1) --C═C(R¹³)--N═C(R¹³)--C(R¹³)═C(R¹³)--, 2) --C═C(R¹³)--C(R¹³)═N--C(R¹³)═C(R¹³)--, 3) --C═C(R¹³)--N═C(R¹³)--N═C(R¹³)--, 4) --C═N--C(R¹³)═C(R¹³)--C(R¹³)═N--, or 5) --C═N--C(R¹³)═N--C(R¹³)═C(R¹³)--; ##STR181## is as defined above; ##STR182## is as defined above; or ##STR183## wherein G is S; R² is a) --(C₁ -C₁₂ alkyl)--X, or ##STR184## X is a) halogen (F, Cl, Br, I), b) --CN, c) --NHR¹⁴ d) --NHC(NH)H, e) --NHC(NH)NHR¹⁴, f) --C(NH)NHR¹⁴, g) --OR¹⁴, or h) --SC(═NH)NHR¹⁴ ; R¹¹ is H; R¹³ isH, halogen (F, Cl, Br, I), --(CH₂)_(w) NO₂, (C₁ -C₆)alkyl, --(CH₂)_(r) --D, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CO₂ R³, --(CH₂) _(w) NR⁸ R³, --(CH₂)_(w) S(O)₂ R⁷, --(CH₂ wSO2NHCO--(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO2-phenyl-(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-perfluoroalkyl, --(CH₂)_(w) CN₄ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(t) CN, --NH(CH₂)_(t) CN, --S(CH₂)_(t) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), or --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸ ; R¹⁴ is --H; R¹⁸ and R¹⁹ are independentlyH, halo (F, Cl, Br, I), C₁ -C₆ -alkyl, --(CH₂)_(w) --OR⁸, --(CH₂)_(w) CN, --(CH₂)_(w) NC, --(CH₂)_(w) NO₂, --(CH₂)_(w) S(O)_(r) R⁷, --(CH₂)_(w) NR⁸ R⁹, --(CH₂)_(w) COR⁸, --(CH₂)_(w) CO₂ R⁸, --(CH₂)_(w) CONR⁸ R⁹, --(CH₂)_(w) SO₂ NH--(C₁ -C₅)-alkyl, --(CH₂)_(w) SO₂ NH₂, --(CH₂)_(w) SO₂ NH--CO--(C₁ -C₆)-alkyl, --(CH₂)_(w) SO₂ NH--CO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)-alkyl, --(CH₂)_(w) NHSO₂ --(C₁ -C₆)perfluoroalkyl, --(CH₂)_(w) NHSO₂ -phenyl, --(CH₂)_(w) NHSO₂ -perfluorophenyl, --(CH₂)_(w) CN₄ H, --O(C═O)--(C₁ -C₅ -alkyl), --O(CH₂)_(t) CN, --NH(CH₂)_(t) CN, --S(CH₂)_(t) CN, --(CH₂)_(w) NH--CO--(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -perfluoroalkyl), --(CH₂)_(w) NH--CO--(C₁ -C₆ -phenyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -alkyl), --(CH₂)_(w) NH--CO₂ --(C₁ -C₆ -phenyl), or --O(C═O)phenyl; R18 and R19 can be taken together to form a methylenedioxy group; R²⁰ is selected from the group consisting of:(CH₂)_(r) --D, or --(CH₂)_(u) phenyl wherein the phenyl contains 0-3 substituents selected from R¹⁸ ;and all other required substituents of formula (I) are defined as in claim
 3. 5. A compound of claim 4 selected from the group consisting of:[N¹ -(4-phenylbenzoyl)-(R)-boroarginine, hydrochloride; N¹ -(3-phenoxybenzoyl)-(R)-boroarginine, hydrochloride; N¹ -(1-fluorenonyl)-(R)-boroarginine, hydrochloride N¹ -(4-[1-butyl]benzoyl)-(R)-boroarginine, hydrochloride; N¹ -(2-benzoylbenzoyl)-(R)-boroarginine, hydrochloride;] N¹ -(5-phenyl-2-furoyl)-(R)-boroarginine, hydrochloride; N¹ -(2-phenyl-4-isoquinoloyl)-(R)-boroarginine, hydrochloride; N¹ -(2-methyl-4-phenylbenzoyl)-(R)-boroarginine, hydrochloride; N¹ -[4-phenyl-2-nitrobenzoyl]boroArg, (+)-pinanediol ester; N¹ -[4-phenyl-2-fluorobenzoyl]boroArg, (+)-pinanediol ester; N¹ -[4-phenyl-2-aminobenzoyl]boroArg, (+)-pinanediol ester; N¹ -[4-phenyl-2-(methylsulfonamido)benzoyl]boroArg, (+)-pinanediol ester; N¹ -[4-phenyl-2-(cyanomethylamino)benzoyl]boroArg, (+)-pinanediol ester; N¹ -[4-phenyl-2-(cyanomethyl)benzoyl]boroArg, (+)-pinanediol ester; N¹ -[4-phenyl-2-(diethylamino)benzoyl]boroArg, (+)-pinanediol ester; N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg, (+)pinanediol ester; N¹ -[4-[2-(aminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg, (+)pinanediol ester; N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg, (+)-pinanediol ester; N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]benzoyl]boroArg, (+)-pinanediol ester; N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]benzoyl]boroArg-OH; N¹ -[4-[2-(n-butoxycarbonylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg, (+)-pinanediol ester; N¹ -[4-[2-(diethylaminosulfonyl)phenyl]-2-methyl-benzoyl]boroArg, (+)pinanediol ester; N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-fluorobenzoyl]boroArg, (+)pinanediol ester; N¹ -[4-[2-(aminosulfonyl)phenyl]-2-fluoro-benzoyl]boroArg, (+)pinanediol ester; N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-fluorobenzoyl]boroArg, (+)-pinanediol ester; N¹ -[4-[2-(t-butylaminosulfonyl)phenyl]-2-nitrobenzoyl]boroArg, (+)pinanediol ester; N¹ -[4-[2-(aminosulfonyl)phenyl]-2-nitro-benzoyl]boroArg, (+)pinanediol ester; N¹ -[4-[2-(methoxycarbonylaminosulfonyl)phenyl]-2-nitrobenzoyl]boroArg, (+)-pinanediol ester; N¹ -(3-phenylbenzoyl)boroarg, (+)-pinanediol; N¹ -[4-(3-BOCNHphenyl)2-methyl-benzoyl]boroarg, (+)-pinanediol;] N¹ -(5-phenyl-2-furoyl)boroarg, (+)-pinanediol; N¹ -(5-phenyl-2-thienyl)boroarg, (+)-pinanediol; N¹ -[4-(3-aminophenyl)benzoyl]boroarg, (+)-pinanediol; N¹ -(3-phenylbenzoyl)borolys, (+)-pinanediol;] N¹ -(5-phenyl-2-furoyl )boroarg-OH; (R)-[5-amino-1-[[[5-(phenylmethyl)-1H -1,2,4-triazol -1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride; [3aS-[2(S*),3aα,4β, 6β]]-(1,1-dimethylethyl) [3-[5-[[[4-[(amino-iminomethyl)amino]-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzo-dioxaborol-2-yl)butyl]amino]carbonyl]-2-thienyl]phenyl]carbamate hydrochloride; [3aS -[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-5-(phenyl-methyl)-3-(2H -tetrazol-5-ylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-1-[2-[[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]amino]-2-oxoethyl]-5-(phenylmethyl)-1H -1,2,4-triazole-3-acetic acid hydrochloride 1:1; [3aS-[2(S*),3aα,4β,6β,7aβ]]-1-[2-[[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]amino]-2-oxoethyl]-3-(phenylmethyl)-1H-1,2,4-triazole-5-acetic acid hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-methyl 1-[2-[[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-amino]-2-oxoethyl]-5-(phenylmethyl)-1H-1,2,4-triazole-3-acetate hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα,]]-methyl 1-[2-[[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-amino]-2-oxoethyl]-3-(phenylmethyl)-1H-1,2,4-triazole-5-acetate hydrochloride; [3aS [2(S*), 3aα,4β, 6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3-phenyl-5-(phenyl-methyl)-1H -1,2,4-triazole-1-acetamide hydrochloride; (R)-[5-amino-1-[[[3-phenyl-5-(phenylmethyl)-1H-1,2,4-triazol-1-yl]acetyl]-amino]pentyl]boronic acid hydrochloride; [3aS-[2(S*),3α,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3-(3-nitro-phenyl)-5-(phenylmethyl)-1H -1,2,4-triazole-1-acetamide hydrochloride; [3aS-[2(S*),3aα,4α, 6β,7aα]]-N-[4-[(aminoiminomethyl)-amino]-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)butyl]-3-(3-nitrophenyl)-5-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα9 ]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3,5-bis(phenyl-methyl)-1H-1,2,4-triazole-1-acetamide hydrochloride; [3aS-[2(S*),3a,4β,6β,7aα]]-N-[4-[(aminoiminomethyl)-amino]-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)butyl]-3,5-bis(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide; (R)-[5-amino-1-[[[3-(phenylmethyl)-1H-1,2,4-triazol-1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride; [3aS-[2(S*), 3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl]-5-methyl-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride; [3aS-[2(R*),3aα,4β,6β]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-5-[(phenyl-methoxy)methyl]-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl]-5-(cyanomethyl)-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride; 3aS-[2(S*), 3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-3-(phenylmethyl)-5-propyl-1H-1,2,4-triazole-1-acetamide hydrochloride; [3aS-[2(S*),3aα,4β, 6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl]-5-phenyl-3-(phenylmethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride; (R)-[5-amino-1-[[[5-methyl-3-(phenylmethyl)-1H-1,2,4-triazol-1-yl]acetyl]-amino]pentyl]boronic acid hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl]-3-phenyl-1H-1,2,4-triazole-1-acetamide hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl]-5-methyl-3-phenyl-1H-1,2,4-triazole-1-acetamide hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)pentyl]-5-(2-phenyl-ethyl)-1H-1,2,4-triazole-1-acetamide; (R)-[5-amino-1-[[[5-(2-phenylethyl)-1H-1,2,4-triazol-1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl]-3,5-bis(2-phenyl-ethyl)-1H-1,2,4-triazole-1-acetamide hydrochloride; (R)-[5-amino-1-[[[3,5-bis(2-phenylethyl)-1H -1,2,4-triazol-1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl]-3-(2-phenylethyl)-1H-1,2,4-triazole-1-acetamide; (R)-[5-amino-1-[[[3-(2-phenylethyl)-1H-1,2,4-triazol-1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl]-3-(3-phenyl-propyl)-1H-1,2,4-triazole-1-acetamide; (R)-[5-amino-1-[[[5-(3-phenylpropyl)-1H-1,2,4-triazol-1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride; (R)-[5-amino-1-[[[3-(3-phenylpropyl)-1H-1,2,4-triazol-1-yl]acetyl]amino]-pentyl]boronic acid hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl]-1,5-bis(phenyl-methyl)-1H -1,2,4-triazole-3-acetamide hydrochloride 2:8; (R)-[5-amino-1-[[[1,5-bis (phenylmethyl)-1H-1,2,4-triazol-3-yl]acetyl]amino]pentyl]boronic acid hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a, 5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl]-4-methyl-2-phenyl-5-pyrimidinecarboxamide hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimetyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl]-2,4-diphenyl-5-pyrimidinecarboxamide hydrochloride; [3aS-[2(S*),3aα,4β,6β,7aα]]-N-[4-[(amimoiminomethyl)amino]-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl)-butyl]-4-methyl-2-phenyl-5-pyrimidinecarboxamide hydrochloride; [3aS-[2(S*),3α,4β,6β,7aα]]-N-[5-amino-1-(hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl) pentyl]-6-phenyl-3-pyridinecarboxamide hydrochloride and (R)-[5-amino-1-[[(6-phenyl-3-pyridinyl) carbonyl]amino]pentyl]boronic acid dihydrochloride.
 6. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of any one of claims 1 through
 5. 7. A method of treating a physiological disorder in a warm blooded animal catalyzed by trypsin-like enzymes comprising administering to an animal in need of such treatment an effective amount of a compound of any one of claims 1 through
 5. 